Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions

Pd-catalyzed cross-coupling reactions that form C–N bonds have become useful methods to synthesize anilines and aniline derivatives, an important class of compounds throughout chemical research. A key factor in the widespread adoption of these methods has been the continued development of reliable and versatile catalysts that function under operationally simple, user-friendly conditions. This review provides an overview of Pd-catalyzed N-arylation reactions found in both basic and applied chemical research from 2008 to the present. Selected examples of C–N cross-coupling reactions between nine classes of nitrogen-based coupling partners and (pseudo)aryl halides are described for the synthesis of heterocycles, medicinally relevant compounds, natural products, organic materials, and catalysts.

[1]  T. J. Carlin,et al.  Bioinspired Synthesis of a Sedaxane Metabolite Using Catalytic Vanadyl Acetylacetonate and Molecular Oxygen. , 2015, The Journal of organic chemistry.

[2]  J. Hartwig,et al.  Palladium‐Catalyzed Arylation of Fluoroalkylamines. , 2015 .

[3]  R. Froese,et al.  Selective Monoarylation of Primary Amines Using the Pd‐PEPPSI‐IPentCl Precatalyst. , 2015 .

[4]  T. Colacot,et al.  Reactions of the 21st Century: Two Decades of Innovative Catalyst Design for Palladium-Catalyzed Cross-Couplings , 2015 .

[5]  D. Schollmeyer,et al.  Palladium-catalyzed domino C-H/N-H functionalization: an efficient approach to nitrogen-bridged heteroacenes. , 2015, Chemistry.

[6]  J. McCarter,et al.  The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors. , 2015, Bioorganic & medicinal chemistry letters.

[7]  Nicolas Joubert,et al.  Palladium-Catalyzed Amination of N-Free 2-Chloro-7-azaindole. , 2015, Organic letters.

[8]  R. Froese,et al.  Selective Monoarylation of Primary Amines Using the Pd-PEPPSI-IPent(Cl) Precatalyst. , 2015, Angewandte Chemie.

[9]  Siv Lise Bedringaas,et al.  4-Alkylated Silver–N-Heterocyclic Carbene (NHC) Complexes with Cytotoxic Effects in Leukemia Cells , 2015, ChemMedChem.

[10]  D. Gündisch,et al.  The twin drug approach for novel nicotinic acetylcholine receptor ligands. , 2015, Bioorganic & medicinal chemistry.

[11]  S. Buchwald,et al.  In-Depth Assessment of the Palladium-Catalyzed Fluorination of Five-Membered Heteroaryl Bromides , 2015, Organometallics.

[12]  Tyler B Fleetham,et al.  Efficient Red-Emitting Platinum Complex with Long Operational Stability. , 2015, ACS applied materials & interfaces.

[13]  Y. Nakayama,et al.  An Efficient Synthesis of N-(Hetero)arylcarbazoles: Palladium-Catalyzed Coupling Reaction between (Hetero)aryl Chlorides and N-Carbazolylmagnesium Chloride , 2015 .

[14]  C. Oliver Kappe,et al.  Continuous-Flow Technology — A Tool for the Safe Manufacturing of Active Pharmaceutical Ingredients , 2015 .

[15]  Thomas J. Colacot,et al.  Generating Active "L-Pd(0)" via Neutral or Cationic π-Allylpalladium Complexes Featuring Biaryl/Bipyrazolylphosphines: Synthetic, Mechanistic, and Structure-Activity Studies in Challenging Cross-Coupling Reactions. , 2015, The Journal of organic chemistry.

[16]  D. González‐Rodríguez,et al.  G-arylated hydrogen-bonded cyclic tetramer assemblies with remarkable thermodynamic and kinetic stability. , 2015, Organic letters.

[17]  J. Carrick,et al.  Pd-Catalyzed Diamination of 1,2,4-Triazinyl Complexant Scaffolds. , 2015, The Journal of organic chemistry.

[18]  E. V. D. Eycken,et al.  Metal‐Mediated Post‐Ugi Transformations for the Construction of Diverse Heterocyclic Scaffolds , 2015 .

[19]  D. González‐Rodríguez,et al.  High-fidelity noncovalent synthesis of hydrogen-bonded macrocyclic assemblies. , 2015, Angewandte Chemie.

[20]  David Cantillo,et al.  Continuous-flow technology—a tool for the safe manufacturing of active pharmaceutical ingredients. , 2015, Angewandte Chemie.

[21]  Robert M. Edkins,et al.  Synthesis and photophysics of a 2,7-disubstituted donor-acceptor pyrene derivative: an example of the application of sequential Ir-catalyzed C-H borylation and substitution chemistry. , 2015, The Journal of organic chemistry.

[22]  H. Knölker,et al.  Total syntheses of murrayamine E, I, and K. , 2015, The Journal of organic chemistry.

[23]  Young Kwan Kim,et al.  Synthesis and electroluminescent properties of 9,10-diphenylanthracene containing 9H-carbazole derivatives for blue organic light-emitting diodes , 2015 .

[24]  F. Emery,et al.  Pd(II)-mediated cyclodehydrogenation of formyldiarylamines—total synthesis of natural carbazoles clauraila A, clausenal and 6-methoxymurrayanine , 2015 .

[25]  Hyeung‐geun Park,et al.  Synthesis and optimization of picolinamide derivatives as a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. , 2015, Bioorganic & medicinal chemistry letters.

[26]  D. Gray,et al.  Donor−Acceptor Type Thioxanthones: Synthesis, Optical Properties, and Two-Photon Induced Polymerization , 2015 .

[27]  Nathaniel H. Park,et al.  Design of New Ligands for the Palladium-Catalyzed Arylation of α-Branched Secondary Amines. , 2015, Angewandte Chemie.

[28]  J. Sperry,et al.  Total Synthesis of (—)‐Aspergilazine A. , 2015 .

[29]  T. Cailly,et al.  A General Synthesis of Diversely Substituted Indazoles and Hetero-Aromatic Derivatives from O-Halo-(het)arylaldehydes or -phenones. , 2015 .

[30]  Jianbo Hou,et al.  Development of Improved Amidoquinoline Polyolefin Catalysts with Ultrahigh Molecular Weight Capacity , 2015 .

[31]  E. V. Van der Eycken,et al.  Metal-mediated post-Ugi transformations for the construction of diverse heterocyclic scaffolds. , 2015, Chemical Society reviews.

[32]  Chao‐Ping Hsu,et al.  Synthesis and isolation of an acyclic tridentate bis(pyridine)carbodicarbene and studies on its structural implications and reactivities. , 2015, Angewandte Chemie.

[33]  S. Buchwald,et al.  Rational Ligand Design for the Arylation of Hindered Primary Amines Guided by Reaction Progress Kinetic Analysis , 2015, Journal of the American Chemical Society.

[34]  F. Svensson,et al.  Efficient and Selective Palladium-Catalysed C-3 Urea Couplings to 3,5-Dichloro-2(1H)-pyrazinones , 2015 .

[35]  S. Messaoudi,et al.  2-Aminobiphenyl Palladacycles: The “Most Powerful” Precatalysts in C–C and C–Heteroatom Cross-Couplings , 2015 .

[36]  J. N. Moorthy,et al.  Amorphous host materials based on Tröger's base scaffold for application in phosphorescent organic light-emitting diodes. , 2015, ACS applied materials & interfaces.

[37]  C. O'bryan,et al.  Integrated cross-coupling strategy for an α-carboline-based Aurora B kinase inhibitor. , 2015, The Journal of organic chemistry.

[38]  S. Messaoudi,et al.  Synthesis of fused 1-aminoindole polycycles by a sequence of palladium-catalyzed N–H and C(sp2)–H arylations. , 2015, The Journal of organic chemistry.

[39]  N. Luedtke,et al.  Fluorescent probe for proton-coupled DNA folding revealing slow exchange of i-motif and duplex structures. , 2015, Journal of the American Chemical Society.

[40]  D. B. Duignan,et al.  Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit. , 2015, Journal of medicinal chemistry.

[41]  T. Kano,et al.  Design and Synthesis of a Biphenyl‐Based Chiral Amino Sulfonamide with High Catalytic Performance in Mannich Reactions. , 2014 .

[42]  X. Zhang,et al.  Chemoselective Amination of Propargylic C(sp3)—H Bonds by Cobalt(II)‐Based Metalloradical Catalysis. , 2014 .

[43]  J. Yao,et al.  Strongly coupled cyclometalated ruthenium-triarylamine hybrids: tuning electrochemical properties, intervalence charge transfer, and spin distribution by substituent effects. , 2014, Chemistry.

[44]  William J. Potscavage,et al.  Anthraquinone-based intramolecular charge-transfer compounds: computational molecular design, thermally activated delayed fluorescence, and highly efficient red electroluminescence. , 2014, Journal of the American Chemical Society.

[45]  K. Walldén,et al.  2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion , 2014, Bioorganic & medicinal chemistry.

[46]  Siew K. Yeap,et al.  Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation , 2014, Journal of medicinal chemistry.

[47]  B. A. Chalmers,et al.  TMIO-PyrImid hybrids are profluorescent, site-directed spin labels for nucleic acids. , 2014, Organic letters.

[48]  U. Bunz,et al.  A persistent diazaheptacene derivative. , 2014, Journal of the American Chemical Society.

[49]  J. T. Njardarson,et al.  Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. , 2014, Journal of medicinal chemistry.

[50]  E. V. D. Eycken,et al.  Regio‐ and Chemoselective Formation of Spiroindolinone–Isoindolinone by a Palladium‐Catalyzed Buchwald–Hartwig Addition–Elimination Sequence , 2014 .

[51]  Manman Sun,et al.  One-pot synthesis of 1,2-diphenyl-1H-benzo[d]imidazole derivatives by a Pd-catalyzed N-arylation and Cu-catalyzed C–H functionalization/C–N bond formation process , 2014 .

[52]  Christophe Simon,et al.  The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. , 2014, Journal of medicinal chemistry.

[53]  J. Sperry,et al.  Total synthesis of (-)-aspergilazine A. , 2014, Organic letters.

[54]  M. Blanchard‐Desce,et al.  Two-photon-induced fluorescence in new π-expanded diketopyrrolopyrroles. , 2014, Chemistry.

[55]  Wenjing Chu,et al.  Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. , 2014, Journal of medicinal chemistry.

[56]  T. Q. Hung,et al.  Efficient Synthesis of Biscarbazoles by Palladium-Catalyzed Twofold C—N Coupling and C—H Activation Reactions. , 2014 .

[57]  Na Ye,et al.  Palladium-catalyzed N-arylation of 2-aminobenzothiazole-4- carboxylates/carboxamides: facile synthesis of PARP14 inhibitors , 2014 .

[58]  M. Mizuno,et al.  Rapid access to diverse α-carbolines through sequential transition metal catalyzed amination and direct C–H arylation , 2014 .

[59]  Yanxing Jia,et al.  Total Synthesis of Dictyodendrins B and E, and Formal Synthesis of Dictyodendrin C , 2014 .

[60]  A. Caron,et al.  Synthesis of a Carprofen Analogue Using a Continuous Flow UV-Reactor , 2014 .

[61]  T. Nakatsuka,et al.  Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors. , 2014, Journal of medicinal chemistry.

[62]  A. Hoveyda,et al.  Synthesis of (±)-tetrapetalone A-Me aglycon. , 2014, Angewandte Chemie.

[63]  H. Kasai,et al.  Caged glutamates with π-extended 1,2-dihydronaphthalene chromophore: design, synthesis, two-photon absorption property, and photochemical reactivity. , 2014, The Journal of organic chemistry.

[64]  H. El‐Nezami,et al.  Molecular imaging of peroxynitrite with HKGreen-4 in live cells and tissues. , 2014, Journal of the American Chemical Society.

[65]  A. Gupta,et al.  Mechanistic Insights into the Palladium‐Catalyzed Domino Synthesis of 10,11‐Dihydro‐5H‐dibenzo[b,e][1,4]diazepines , 2014 .

[66]  M. Liang,et al.  Novel triphenylamine donors with carbazole moieties for organic sensitizers toward cobalt(II/III) redox mediators. , 2014, Organic letters.

[67]  Srinivasan A Kaliyaperumal,et al.  Palladium mediated intramolecular multiple C-X/C-H cross coupling and C-H activation: synthesis of carbazole alkaloids calothrixin B and murrayaquinone A. , 2014, Organic & biomolecular chemistry.

[68]  E. V. Van der Eycken,et al.  Facile access to functionalized spiro[indoline-3,2'-pyrrole]-2,5'-diones via post-Ugi domino Buchwald-Hartwig/Michael reaction. , 2014, Organic letters.

[69]  L. Liao,et al.  Control of conjugation degree via position engineering to highly efficient phosphorescent host materials. , 2014, Organic letters.

[70]  H. Knölker,et al.  Palladium(II)-Catalyzed Synthesis of the Formylcarbazole Alkaloids Murrayaline A–C, 7-Methoxymukonal, and 7-Methoxy-O-methylmukonal† , 2014 .

[71]  E. Moran,et al.  Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD. , 2014, Bioorganic & medicinal chemistry letters.

[72]  X. Zhang,et al.  Chemoselective amination of propargylic C(sp³)-H bonds by cobalt(II)-based metalloradical catalysis. , 2014, Angewandte Chemie.

[73]  B. Feringa,et al.  Dual stereocontrol over the Henry reaction using a light- and heat-triggered organocatalyst. , 2014, Chemical communications.

[74]  J. Kehler,et al.  Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands. , 2014, Journal of medicinal chemistry.

[75]  P. Chou,et al.  Indolo[2,3-b]carbazole synthesized from a double-intramolecular Buchwald-Hartwig reaction: its application for a dianchor DSSC organic dye. , 2014, Organic letters.

[76]  S. Buchwald,et al.  Regioselective Synthesis of Benzimidazolones via Cascade C–N Coupling of Monosubstituted Ureas , 2014, Organic letters.

[77]  P. Lam,et al.  2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists. , 2014, Bioorganic & medicinal chemistry letters.

[78]  Young Chan Kim,et al.  o-Methoxy substituents in spiro-OMeTAD for efficient inorganic-organic hybrid perovskite solar cells. , 2014, Journal of the American Chemical Society.

[79]  A. J. Briggs,et al.  A Scalable Route to an Unusual 3,3-Dimethyl-2,3-dihydrobenzofuran Ring System Present in an HCV Drug Candidate , 2014 .

[80]  E. Laird,et al.  Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase. , 2014, Bioorganic & medicinal chemistry letters.

[81]  K. Ashton,et al.  Nonracemic synthesis of GK-GKRP disruptor AMG-3969. , 2014, The Journal of organic chemistry.

[82]  Liang Zhao,et al.  Synthesis, structure, and fullerene-complexing property of azacalix[6]aromatics. , 2014, The Journal of organic chemistry.

[83]  A. W. Schmidt,et al.  First Total Synthesis of Murrastifoline B and an Improved Route to Murrastifoline F , 2014, Synlett.

[84]  M. Yoshizawa,et al.  A solvato-fluorochromic macrocycle of multiple anthracene fluorophores in close proximity. , 2014, Chemistry, an Asian journal.

[85]  S. Buchwald,et al.  N-Substituted 2-Aminobiphenylpalladium Methanesulfonate Precatalysts and Their Use in C–C and C–N Cross-Couplings , 2014, The Journal of organic chemistry.

[86]  T. Q. Hung,et al.  Efficient synthesis of biscarbazoles by palladium-catalyzed twofold C-N coupling and C-H activation reactions. , 2014, Organic & biomolecular chemistry.

[87]  J. Kehler,et al.  New Palladium-Catalyzed Domino Reaction with Intramolecular Ring Closure of an N-(2-Chloro-3-heteroaryl)arylamide: First Synthesis of Oxazolo[4,5-b]pyrazines , 2014 .

[88]  Qun Liu,et al.  Palladium-catalyzed C-S activation/aryne insertion/coupling sequence: synthesis of functionalized 2-quinolinones. , 2014, Angewandte Chemie.

[89]  Bin Li,et al.  Modular synthesis of benzimidazole-fused phenanthridines from 2-arylbenzimidazoles and o-dibromoarenes by a palladium-catalyzed cascade process. , 2014, Organic letters.

[90]  F. Clerici,et al.  2-Amino-3-(phenylsulfanyl)norbornane-2-carboxylate: an appealing scaffold for the design of Rac1-Tiam1 protein-protein interaction inhibitors. , 2014, Journal of medicinal chemistry.

[91]  Hong Liu,et al.  Rapid generation of privileged substructure-based compound libraries with structural diversity and drug-likeness. , 2014, ACS combinatorial science.

[92]  Adam J Rosenberg,et al.  Copper- and palladium-catalyzed amidation reactions for the synthesis of substituted imidazo[4,5-c]pyridines. , 2014, The Journal of organic chemistry.

[93]  W. Denny,et al.  Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3). , 2014, Bioorganic & medicinal chemistry.

[94]  E. O'brien,et al.  Development of a Scalable Synthesis of a Bruton’s Tyrosine Kinase Inhibitor via C–N and C–C Bond Couplings as an End Game Strategy , 2014 .

[95]  S. Buchwald,et al.  Palladium-Catalyzed Amination of Unprotected Five-Membered Heterocyclic Bromides , 2014, Organic letters.

[96]  J. E. Robinson,et al.  Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability. , 2014, ACS medicinal chemistry letters.

[97]  Cory Valente,et al.  Carbon–Heteroatom Coupling Using Pd-PEPPSI Complexes , 2014 .

[98]  J. Neumeyer,et al.  Preliminary pharmacological evaluation of enantiomeric morphinans. , 2014, ACS chemical neuroscience.

[99]  Song Li,et al.  Syntheses of fused tetracyclic quinolines via Ugi-variant MCR and Pd-catalyzed bis-annulation. , 2014, The Journal of organic chemistry.

[100]  X. Pu,et al.  Regiospecific N-heteroarylation of amidines for full-color-tunable boron difluoride dyes with mechanochromic luminescence. , 2013, Angewandte Chemie.

[101]  H. Oki,et al.  Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors. , 2013, Bioorganic & medicinal chemistry.

[102]  David M. Shackleford,et al.  Two Analogues of Fenarimol Show Curative Activity in an Experimental Model of Chagas Disease , 2013, Journal of medicinal chemistry.

[103]  A. K. Muthusamy,et al.  Efficient synthesis and in vivo incorporation of acridon-2-ylalanine, a fluorescent amino acid for lifetime and Förster resonance energy transfer/luminescence resonance energy transfer studies. , 2013, Journal of the American Chemical Society.

[104]  Heung-Jin Choi,et al.  C3v-Symmetric tripodal nitrophenylurea based anion receptors built on structurally preorganized trindane scaffold , 2013 .

[105]  M. Stradiotto,et al.  BippyPhos: a single ligand with unprecedented scope in the Buchwald-Hartwig amination of (hetero)aryl chlorides. , 2013, Chemistry.

[106]  K. Zhuo,et al.  One-Pot Synthesis of Benzimidazo(1,2-f)phenanthridines by Cascade Palladium-Catalyzed N-Arylation and Intramolecular C-H Coupling , 2013 .

[107]  D. Friedrich,et al.  A Convenient Preparation of Thieno[3,2-c]pyrazole , 2013 .

[108]  E. V. Van der Eycken,et al.  C-N bond forming cross-coupling reactions: an overview. , 2013, Chemical Society reviews.

[109]  S. Laufer,et al.  Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood. , 2013, Journal of medicinal chemistry.

[110]  S. Höger,et al.  Fluctuating exciton localisation in giant pi-conjugated spoked-wheel macrocycles , 2015, 1507.06536.

[111]  Dongbing Zhao,et al.  Palladium-catalyzed tandem N-H/C-H arylation: regioselective synthesis of N-heterocycle-fused phenanthridines as versatile blue-emitting luminophores. , 2013, Organic & biomolecular chemistry.

[112]  S. Buchwald,et al.  Cascade palladium catalysis: a predictable and selectable regiocontrolled synthesis of N-arylbenzimidazoles. , 2013, Angewandte Chemie.

[113]  D. Fichou,et al.  Synthesis, properties, and remarkable 2 D Self-Assembly at the Liquid/Solid interface of a series of triskele-shaped 5,11,17-triazatrinaphthylenes (TrisK). , 2013, Chemistry.

[114]  Keisuke Suzuki,et al.  Synthesis and determination of the absolute configuration of cavicularin by a symmetrization/asymmetrization approach. , 2013, Angewandte Chemie.

[115]  Andreas Kirschning,et al.  Heating under high-frequency inductive conditions: application to the continuous synthesis of the neurolepticum olanzapine (Zyprexa). , 2013, Angewandte Chemie.

[116]  Klaus Meerholz,et al.  Solution processed organic double light-emitting layer diode based on cross-linkable small molecular systems. , 2013, Angewandte Chemie.

[117]  Takayoshi Suzuki,et al.  A reductant-resistant and metal-free fluorescent probe for nitroxyl applicable to living cells. , 2013, Journal of the American Chemical Society.

[118]  Frederik J. R. Rombouts,et al.  Complementary Regioselectivity in Rh(III)‐Catalyzed Insertions of Potassium Vinyltrifluoroborate via C—H Activation: Preparation and Use of 4‐Trifluoroboratotetrahydroisoquinolones. , 2013 .

[119]  D. Lietha,et al.  Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity. , 2013, Bioorganic & medicinal chemistry letters.

[120]  David A. Scott,et al.  Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. , 2013, Bioorganic & medicinal chemistry letters.

[121]  Krupal P. Jethava,et al.  Palladium-catalyzed regio- and chemoselective ortho-benzylation of C-H bond using a functionalizable primary amide directing group: a concise synthesis of dibenzo[b,e]azepin-6-ones. , 2013, Chemical communications.

[122]  Shuang Gao,et al.  Asymmetric epoxidation of alkenes catalyzed by a porphyrin-inspired manganese complex. , 2013, Organic letters.

[123]  G. Piersanti,et al.  Synthesis of (-)-epi-indolactam V by an intramolecular Buchwald-Hartwig C-N coupling cyclization reaction. , 2013, The Journal of organic chemistry.

[124]  J. Molnár,et al.  Synthesis and pharmacological investigation of new N-hydroxyalkyl-2-aminophenothiazines exhibiting marked MDR inhibitory effect. , 2013, Bioorganic & medicinal chemistry.

[125]  S. Buchwald,et al.  Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts. , 2013, Organic letters.

[126]  M. Poyatos,et al.  Triphenylene-based tris(N-heterocyclic carbene) ligand: unexpected catalytic benefits. , 2013, Angewandte Chemie.

[127]  Toshiyuki Watanabe,et al.  Hinge-Linked Polymer Gels: A Rigid Network Cross-Linked with a Rotatable Tetrasubstituted Ferrocene , 2013 .

[128]  Amanda L. Weeks,et al.  Synthesis of murrayaquinone A and analogues via ring-closing C–H arylation , 2013 .

[129]  Adam R. Johnson,et al.  Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. , 2013, Journal of medicinal chemistry.

[130]  Yanxing Jia,et al.  Total synthesis of dictyodendrins B and E. , 2013, The Journal of organic chemistry.

[131]  V. Cody,et al.  Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles. , 2013, Journal of medicinal chemistry.

[132]  Qing Xiang,et al.  Design and synthesis of 2-N-substituted indazolone derivatives as non-carboxylic acid glycogen synthase activators. , 2013, Bioorganic & medicinal chemistry letters.

[133]  L. Wojtas,et al.  Effective synthesis of chiral N-fluoroaryl aziridines through enantioselective aziridination of alkenes with fluoroaryl azides. , 2013, Angewandte Chemie.

[134]  James A. Wright,et al.  A Practical Synthesis of an Aminopyridine as a Component of a BTK Inhibitor , 2013 .

[135]  Gerald W. Shipps,et al.  Structure-based design and optimization of 2-aminothiazole-4-carboxamide as a new class of CHK1 inhibitors. , 2013, Bioorganic & medicinal chemistry letters.

[136]  S. Buchwald,et al.  Synthesis and application of palladium precatalysts that accommodate extremely bulky di-tert-butylphosphino biaryl ligands. , 2013, Organic letters.

[137]  M. Lautens,et al.  Multicomponent multicatalyst reactions (MC)2R: one-pot synthesis of 3,4-dihydroquinolinones. , 2013, Organic letters.

[138]  T. Ueda,et al.  Planar chiral [2.2]paracyclophane-based bis(thiourea) catalyst: application to asymmetric Henry reaction. , 2013, Chemical communications.

[139]  E. Kool,et al.  Genetically encoded multispectral labeling of proteins with polyfluorophores on a DNA backbone. , 2013, Journal of the American Chemical Society.

[140]  Mi-hyun Kim,et al.  Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects. , 2013, Bioorganic & medicinal chemistry.

[141]  L. Van Meervelt,et al.  Asymmetric Synthesis of 1-Aza-4-deoxypicropodophyllotoxin , 2013, Synlett.

[142]  S. Buchwald,et al.  Highlights from the Flow Chemistry Literature 2013 (Part 1) , 2013, Journal of Flow Chemistry.

[143]  Wesley R. Legant,et al.  Carbofluoresceins and Carborhodamines as Scaffolds for High-Contrast Fluorogenic Probes , 2013, ACS chemical biology.

[144]  R. Álvarez,et al.  Novel symmetrical ureas as modulators of protein arginine methyl transferases. , 2013, Bioorganic & medicinal chemistry.

[145]  S. Buchwald,et al.  Mild and rapid Pd-catalyzed cross-coupling with hydrazine in continuous flow: application to the synthesis of functionalized heterocycles. , 2013, Angewandte Chemie.

[146]  A. Brancale,et al.  Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents. , 2013, Journal of medicinal chemistry.

[147]  L. Altucci,et al.  Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line. , 2013, Bioorganic & medicinal chemistry letters.

[148]  Frederik J. R. Rombouts,et al.  Complementary regioselectivity in Rh(III)-catalyzed insertions of potassium vinyltrifluoroborate via C-H activation: preparation and use of 4-trifluoroboratotetrahydroisoquinolones. , 2013, Organic letters.

[149]  T. Lei,et al.  Azaborine compounds for organic field-effect transistors: efficient synthesis, remarkable stability, and BN dipole interactions. , 2013, Angewandte Chemie.

[150]  J. Senker,et al.  Microporous Functionalized Triazine-Based Polyimides with High CO2 Capture Capacity , 2013 .

[151]  Jun Yeob Lee,et al.  High quantum efficiency blue phosphorescent organic light-emitting diodes using 6-position-modified benzofuro[2,3-b]pyridine derivatives. , 2013, ACS applied materials & interfaces.

[152]  Satoko Baba,et al.  Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands. , 2013, Bioorganic & medicinal chemistry.

[153]  Allan Wu,et al.  Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors. , 2013, Journal of medicinal chemistry.

[154]  Thomas J. Colacot,et al.  An examination of the palladium/Mor-DalPhos catalyst system in the context of selective ammonia monoarylation at room temperature. , 2013, Chemistry.

[155]  K. Thorneloe,et al.  Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema. , 2013, ACS medicinal chemistry letters.

[156]  Roger Guilard,et al.  Colorimetric Hg2+ sensing in water: from molecules toward low-cost solid devices. , 2013, Organic letters.

[157]  Zhijun Zhang,et al.  Synthesis of quinazolin-4(3H)-ones via amidine N-arylation. , 2013, The Journal of organic chemistry.

[158]  S. Peng,et al.  Synthesis, Structure, Magnetism, and Single Molecular Conductance of Linear Trinickel String Complexes with Sulfur‐Containing Ligands , 2013 .

[159]  P. T. Bremer,et al.  Investigating the effects of a hydrolytically stable hapten and a Th1 adjuvant on heroin vaccine performance. , 2012, Journal of medicinal chemistry.

[160]  S. Hecht,et al.  o-Fluoroazobenzenes as readily synthesized photoswitches offering nearly quantitative two-way isomerization with visible light. , 2012, Journal of the American Chemical Society.

[161]  R. Larock,et al.  Synthesis of N-acylcarbazoles through palladium-catalyzed aryne annulation of 2-haloacetanilides. , 2012, The Journal of organic chemistry.

[162]  Yun Liang,et al.  Palladium-catalyzed double N-arylation to synthesize multisubstituted dibenzoazepine derivatives , 2012 .

[163]  Andrei V. Cheprakov,et al.  The Complementary Competitors: Palladium and Copper in C-N Cross-Coupling Reactions , 2012 .

[164]  C. Song,et al.  Asymmetric β-boration of α,β-unsaturated N-acyloxazolidinones by [2.2]paracyclophane-based bifunctional catalyst. , 2012, Organic letters.

[165]  J. Wang,et al.  Auto-Tandem Catalysis: Synthesis of Acridines by Pd-Catalyzed C=C Bond Formation and C(sp2)–N Cross-Coupling , 2012 .

[166]  D. Han,et al.  Design, synthesis, and structure-activity-relationship of phenyl imidazoles as potent Smoothened antagonists. , 2012, Bioorganic & medicinal chemistry letters.

[167]  J. Qin,et al.  Star-shaped hexakis(9,9-dihexyl-9H-fluoren-2-yl)benzene end-capped with carbazole and diphenylamine units: solution-processable, high Tg hole-transporting materials for organic light-emitting devices , 2012 .

[168]  M. Willis,et al.  Palladium-catalyzed synthesis of benzimidazoles and quinazolinones from common precursors. , 2012, The Journal of organic chemistry.

[169]  J. Peyrat,et al.  Palladium-Catalyzed Cross-Coupling of 1-Aminoazoles with Aryl Chlorides: Application to the Synthesis of Unsymmetrical N,N′-Diaryl-1-aminoindoles , 2012 .

[170]  R. Larock,et al.  Palladium-catalyzed annulation of arynes by o-halobenzamides: synthesis of phenanthridinones. , 2012, The Journal of organic chemistry.

[171]  Â. Pinto,et al.  Synthesis of porphyrin indolin-2-one conjugates via palladium-catalyzed amination reactions , 2012 .

[172]  M. Shiro,et al.  A triphenylamine double-decker: from a delocalized radical cation to a diradical dication with an excited triplet state. , 2012, Angewandte Chemie.

[173]  G. S. Singh,et al.  Isatins as privileged molecules in design and synthesis of spiro-fused cyclic frameworks. , 2012, Chemical reviews.

[174]  C. Schwarzinger,et al.  BiIII–Corroles: A Versatile Platform for the Synthesis of Functionalized Corroles , 2012 .

[175]  S. Buchwald,et al.  Catalyst-controlled chemoselective arylation of 2-aminobenzimidazoles. , 2012, Angewandte Chemie.

[176]  Adam J Rosenberg,et al.  Total synthesis of pentosidine. , 2012, Organic letters.

[177]  A. W. Schmidt,et al.  Occurrence, Biogenesis, and Synthesis of Biologically Active Carbazole Alkaloids , 2012 .

[178]  M. Stradiotto,et al.  Addressing challenges in palladium-catalyzed cross-coupling reactions through ligand design. , 2012, Chemistry.

[179]  S. Buchwald,et al.  Design and Preparation of New Palladium Precatalysts for C-C and C-N Cross-Coupling Reactions. , 2012, Chemical science.

[180]  T. Bush,et al.  Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors. , 2012, Bioorganic & medicinal chemistry letters.

[181]  J. J. Farias,et al.  Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor. , 2012, Bioorganic & medicinal chemistry letters.

[182]  Jun Yeob Lee,et al.  N,N-Diphenylpyridin-4-amine as a bipolar core structure of high-triplet-energy host materials for blue phosphorescent organic light-emitting diodes. , 2012, Chemistry, an Asian journal.

[183]  A. Hoveyda,et al.  Synthesis, isolation, characterization, and reactivity of high-energy stereogenic-at-Ru carbenes: stereochemical inversion through olefin metathesis and other pathways. , 2012, Journal of the American Chemical Society.

[184]  L. Kocsis,et al.  Synthesis and photophysical properties of a series of cyclopenta[b]naphthalene solvatochromic fluorophores. , 2012, Journal of the American Chemical Society.

[185]  R. Nagarajan,et al.  Synthesis of pyrido[2,3-b]indoles and pyrimidoindoles via Pd-catalyzed amidation and cyclization. , 2012, Organic & biomolecular chemistry.

[186]  S. Buchwald,et al.  Palladium-catalyzed N-monoarylation of amidines and a one-pot synthesis of quinazoline derivatives. , 2012, Organic letters.

[187]  Melanie H. Wong,et al.  Tri-substituted acylhydrazines as tertiary amide bioisosteres: HCV NS5B polymerase inhibitors. , 2012, Bioorganic & medicinal chemistry letters.

[188]  Katharine K. Duncan,et al.  A novel, unusually efficacious duocarmycin carbamate prodrug that releases no residual byproduct. , 2012, Journal of medicinal chemistry.

[189]  O. Wenger,et al.  Charge delocalization in a homologous series of α,α'-bis(dianisylamino)-substituted thiophene monocations. , 2012, The journal of physical chemistry. A.

[190]  G. Macdonald,et al.  Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. , 2012, Journal of medicinal chemistry.

[191]  Yusuke Nakamura,et al.  Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. , 2012, ACS medicinal chemistry letters.

[192]  L. Fu,et al.  Palladium-catalyzed amidation of aryl halides using 2-dialkylphosphino-2'-alkoxyl-1,1'-binaphthyl as ligands. , 2012, The Journal of organic chemistry.

[193]  C. Garbay,et al.  High yielding microwave-assisted synthesis of tri-substituted 1,3,5-triazines using Pd-catalyzed aryl and heteroarylamination , 2012 .

[194]  Carin C. C. Johansson Seechurn,et al.  Development of Preformed Pd Catalysts for Cross-Coupling Reactions, Beyond the 2010 Nobel Prize , 2012 .

[195]  M. Scharenberg,et al.  Antiadhesion therapy for urinary tract infections--a balanced PK/PD profile proved to be key for success. , 2012, Journal of medicinal chemistry.

[196]  M. Waring,et al.  Room‐Temperature Palladium‐Catalyzed Coupling of Heteroaryl Amines with Aryl or Heteroaryl Bromides. , 2012 .

[197]  K. Kuhen,et al.  Imidazolopiperazines: Lead Optimization of the Second-Generation Antimalarial Agents , 2012, Journal of medicinal chemistry.

[198]  T. Hiyama,et al.  1,4-Bis(diarylamino)-2,5-bis(4-cyanophenylethenyl)benzenes: fluorophores exhibiting efficient red and near-infrared emissions in solid state. , 2012, Angewandte Chemie.

[199]  M. Makishima,et al.  RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists. , 2012, ACS medicinal chemistry letters.

[200]  H. Knölker,et al.  Occurrence, biogenesis, and synthesis of biologically active carbazole alkaloids. , 2012, Chemical reviews.

[201]  Qingle Zeng,et al.  Palladium-catalyzed C-N cross coupling of sulfinamides and aryl halides. , 2012, The Journal of organic chemistry.

[202]  V. S. Rao,et al.  A new cascade reaction: concurrent construction of six and five membered rings leading to novel fused quinazolinones. , 2012, Organic & biomolecular chemistry.

[203]  H. Shinokubo,et al.  Oxidative annulation of β-aminoporphyrins into pyrazine-fused diporphyrins. , 2012, Angewandte Chemie.

[204]  Jinbo Zhao,et al.  Synthesis of imidazo[4,5-b]pyridines and imidazo[4,5-b]pyrazines by palladium catalyzed amidation of 2-chloro-3-amino-heterocycles. , 2012, Organic letters.

[205]  M. McLaughlin,et al.  Process Development and Large-Scale Synthesis of MK-6186, a Non-Nucleoside Reverse Transcriptase Inhibitor for the Treatment of HIV , 2012 .

[206]  Jason J. Hanthorn,et al.  Incorporation of ring nitrogens into diphenylamine antioxidants: striking a balance between reactivity and stability. , 2012, Journal of the American Chemical Society.

[207]  S. Buchwald,et al.  A bulky biaryl phosphine ligand allows for palladium-catalyzed amidation of five-membered heterocycles as electrophiles. , 2012, Angewandte Chemie.

[208]  S. Buchwald,et al.  Palladium-Catalyzed N-Arylation of 2-Aminothiazoles , 2012 .

[209]  Xiaomin Xie,et al.  An Efficient Pd‐Catalyzed Coupling of Hydrazine Derivatives with Aryl Halides. , 2012 .

[210]  B. Maes,et al.  Transition metal-catalyzed N-arylations of amidines and guanidines. , 2012, Chemical Society reviews.

[211]  David K. Leahy,et al.  Development of Two Complementary Syntheses for a Privileged CGRP Receptor Antagonist Substructure , 2012 .

[212]  Michael J. Ferguson,et al.  Rational and predictable chemoselective synthesis of oligoamines via Buchwald-Hartwig amination of (hetero)aryl chlorides employing Mor-DalPhos. , 2012, The Journal of organic chemistry.

[213]  R. Oballa,et al.  Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series. , 2012, Bioorganic & medicinal chemistry letters.

[214]  Courtney A. Cullis,et al.  Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). , 2012, Journal of medicinal chemistry.

[215]  S. Buchwald,et al.  Completely N1-selective palladium-catalyzed arylation of unsymmetric imidazoles: application to the synthesis of nilotinib. , 2012, Journal of the American Chemical Society.

[216]  Marek W. Urban,et al.  Self-repairable copolymers that change color , 2012 .

[217]  O. Baudoin,et al.  Synthesis of tricyclic nitrogen heterocycles by a sequence of palladium-catalyzed N-H and C(sp3)-H arylations. , 2012, Organic letters.

[218]  T. E. Reich,et al.  High CO2 uptake and selectivity by triptycene-derived benzimidazole-linked polymers. , 2012, Chemical communications.

[219]  Nanxin Li,et al.  Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. , 2012, ACS medicinal chemistry letters.

[220]  J. Lai,et al.  Synthesis and optoelectronic properties of novel organosoluble polynorbornenes containing asymmetric pyrenyl and electroactive substituents via ring‐opening metathesis polymerization , 2011 .

[221]  M. Stradiotto,et al.  Palladium-Catalyzed Synthesis of Indoles via Ammonia Cross-Coupling—Alkyne Cyclization. , 2011 .

[222]  R. J. Thomson,et al.  Enantioselective total synthesis and studies into the configurational stability of bismurrayaquinone A. , 2011, Angewandte Chemie.

[223]  Xiaomin Xie,et al.  An Efficient Pd-Catalyzed Couplingof Hydrazine Derivatives with Aryl Halides , 2011 .

[224]  Chetti Prabhakar,et al.  A redox-gated slow-fast-stop molecular rotor. , 2011, Organic letters.

[225]  R. Fröhlich,et al.  Coupling of ortho-substituted aryl chlorides with bulky amides. , 2011, Chemical communications.

[226]  E. Betzig,et al.  Facile and General Synthesis of Photoactivatable Xanthene Dyes , 2011, Angewandte Chemie.

[227]  P. Sunnerhagen,et al.  Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors. , 2011, Journal of medicinal chemistry.

[228]  S. Nolan,et al.  N-Heterocyclic carbene (NHC) ligands and palladium in homogeneous cross-coupling catalysis: a perfect union. , 2011, Chemical Society reviews.

[229]  S. Buchwald,et al.  Concise palladium-catalyzed synthesis of dibenzodiazepines and structural analogues. , 2011, Journal of the American Chemical Society.

[230]  S. Sinning,et al.  Synthesis of 3,7-disubstituted imipramines by palladium-catalysed amination/cyclisation and evaluation of their inhibition of monoamine transporters. , 2011, Chemistry.

[231]  Carin C C Johansson Seechurn,et al.  Air-stable Pd(R-allyl)LCl (L= Q-Phos, P(t-Bu)3, etc.) systems for C-C/N couplings: insight into the structure-activity relationship and catalyst activation pathway. , 2011, The Journal of organic chemistry.

[232]  L. Wojtas,et al.  Highly asymmetric intramolecular cyclopropanation of acceptor-substituted diazoacetates by Co(II)-based metalloradical catalysis: iterative approach for development of new-generation catalysts. , 2011, Journal of the American Chemical Society.

[233]  R. Wilkes,et al.  Scaling up Metal Scavenging Operations for Pharmaceutical Pilot Plant Manufactures , 2011 .

[234]  H. Neumann,et al.  Recyclable catalysts for palladium-catalyzed aminations of aryl halides. , 2011, Chemistry.

[235]  Xin Liu,et al.  Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability. , 2011, Bioorganic & medicinal chemistry letters.

[236]  J. Gisselbrecht,et al.  Diporphyrinylamines: synthesis and electrochemistry. , 2011, Organic letters.

[237]  S. Hecht,et al.  Electronic decoupling approach to quantitative photoswitching in linear multiazobenzene architectures. , 2011, Journal of Physical Chemistry B.

[238]  Riccardo Colombo,et al.  Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. , 2011, Bioorganic & medicinal chemistry letters.

[239]  C. Kappe,et al.  Microwave-assisted and continuous flow multistep synthesis of 4-(pyrazol-1-yl)carboxanilides. , 2011, The Journal of organic chemistry.

[240]  J. Rebek,et al.  A transparent photo-responsive organogel based on a glycoluril supergelator. , 2011, Chemical communications.

[241]  R. Nagarajan,et al.  Synthesis of α‐Carbolines via Pd‐Catalyzed Amidation and Vilsmeier—Haack Reaction of 3‐Acetyl‐2‐chloroindoles. , 2011 .

[242]  K. Kuhen,et al.  Imidazolopiperazines: Hit to Lead Optimization of New Antimalarial Agents , 2011, Journal of medicinal chemistry.

[243]  K. Kunii,et al.  Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. , 2011, Journal of medicinal chemistry.

[244]  Brian J. Kotecki,et al.  A general method for palladium-catalyzed reactions of primary sulfonamides with aryl nonaflates. , 2011, The Journal of organic chemistry.

[245]  G. Fabrizi,et al.  Update 1 of: Synthesis and functionalization of indoles through palladium-catalyzed reactions. , 2011, Chemical reviews.

[246]  Allan M Jordan,et al.  The medicinal chemist's toolbox: an analysis of reactions used in the pursuit of drug candidates. , 2011, Journal of medicinal chemistry.

[247]  S. Buchwald,et al.  Synthesis of unsymmetrical diarylureas via Pd-catalyzed C-N cross-coupling reactions. , 2011, Organic letters.

[248]  J. C. Ruble,et al.  Mild Pd-catalyzed N-arylation of methanesulfonamide and related nucleophiles: avoiding potentially genotoxic reagents and byproducts. , 2011, Organic letters.

[249]  Xiao-yi Xiao,et al.  Synthesis and Antibacterial Activity of Pentacyclines: A Novel Class of Tetracycline Analogs , 2011, Journal of medicinal chemistry.

[250]  S. Ley,et al.  An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals , 2011, Beilstein journal of organic chemistry.

[251]  T. Moore,et al.  Carotenoid photoprotection in artificial photosynthetic antennas. , 2011, Journal of the American Chemical Society.

[252]  H. Bolink,et al.  Solution processable high band gap hosts based on carbazole functionalized cyclic phosphazene cores for application in organic light-emitting diodes , 2011 .

[253]  A. Glas,et al.  Discovery and synthesis of new UV-induced intrastrand C(4-8)G and G(8-4)C photolesions. , 2011, Journal of the American Chemical Society.

[254]  Eliot Sugarman,et al.  Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. , 2011, ACS medicinal chemistry letters.

[255]  M. T. Herrero,et al.  An straightforward entry to new pyrazolo-fused dibenzo[1,4]diazepines. , 2011, Organic & biomolecular chemistry.

[256]  P. Baran,et al.  Total synthesis guided structure elucidation of (+)-psychotetramine. , 2011, Angewandte Chemie.

[257]  Javier Magano,et al.  Large-scale applications of transition metal-catalyzed couplings for the synthesis of pharmaceuticals. , 2011, Chemical reviews.

[258]  R. V. van Montfort,et al.  Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. , 2011, Journal of medicinal chemistry.

[259]  C. Valdés,et al.  Tosylhydrazide-promoted palladium-catalyzed reaction of β-aminoketones with o-dihaloarenes: combining organocatalysis and transition-metal catalysis. , 2011, Angewandte Chemie.

[260]  Mark S. Taylor,et al.  Anion detection by a fluorescent poly(squaramide): self-assembly of anion-binding sites by polymer aggregation. , 2011, Angewandte Chemie.

[261]  L. Wojtas,et al.  Enantioselective cyclopropenation of alkynes with acceptor/acceptor-substituted diazo reagents via Co(II)-based metalloradical catalysis. , 2011, Journal of the American Chemical Society.

[262]  E. Laird,et al.  The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors. , 2011, Bioorganic & medicinal chemistry letters.

[263]  S. Poda,et al.  Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands. , 2011, Bioorganic & medicinal chemistry letters.

[264]  T. Moore,et al.  Mimicking the role of the antenna in photosynthetic photoprotection. , 2011, Journal of the American Chemical Society.

[265]  D. Goldsmith,et al.  Mammalian Target of Rapamycin (mTOR) Inhibitors , 2011, Drug safety.

[266]  M. Nazaré,et al.  A general and mild domino approach to substituted 1-aminoindoles. , 2011, Chemical communications.

[267]  C. Fischer,et al.  Palladium- and copper-mediated N-aryl bond formation reactions for the synthesis of biological active compounds , 2011, Beilstein journal of organic chemistry.

[268]  A. Ting,et al.  Synthesis of 7‐Aminocoumarin by Buchwald–Hartwig Cross Coupling for Specific Protein Labeling in Living Cells , 2011, Chembiochem : a European journal of chemical biology.

[269]  J. Hartwig,et al.  Catalytic organometallic reactions of ammonia. , 2011, Angewandte Chemie.

[270]  M. Sivakumar,et al.  Carbamic acid 2-trimethylsilylethyl ester as a new ammonia equivalent for palladium-catalyzed amination of aryl halides , 2010 .

[271]  F. Fiorentini,et al.  4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. , 2010, Bioorganic & medicinal chemistry letters.

[272]  M. Stradiotto,et al.  Palladium-catalyzed cross-coupling of aryl chlorides and tosylates with hydrazine. , 2010, Angewandte Chemie.

[273]  Simon J F Macdonald,et al.  Factors determining the selection of organic reactions by medicinal chemists and the use of these reactions in arrays (small focused libraries). , 2010, Angewandte Chemie.

[274]  Tohru Sato,et al.  Preparation and characterization of N-anisyl-substituted hexaaza[1(6)]paracyclophane. , 2010, Angewandte Chemie.

[275]  J. Renaud,et al.  Direct amination of aryl halides with ammonia. , 2010, Chemical Society reviews.

[276]  Margaret S. Wu,et al.  Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities. , 2010, Bioorganic & medicinal chemistry letters.

[277]  James B. Thomas,et al.  1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists. , 2010, ACS medicinal chemistry letters.

[278]  R. Andersen,et al.  Synthetic analogues of the microtubule-stabilizing sponge alkaloid ceratamine A are more active than the natural product. , 2010, Journal of medicinal chemistry.

[279]  Chun-Ho Wong,et al.  The effects of microenvironment polarity and dendritic branching of aliphatic hydrocarbon dendrons on the self-assembly of 2-ureido-4-pyrimidinones. , 2010, Chemistry, an Asian journal.

[280]  V. Croci,et al.  Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity. , 2010, Bioorganic & medicinal chemistry.

[281]  J. Vaquero,et al.  Application of Selective Palladium-Mediated Functionalization of the Pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine Heterocyclic System for the Total Synthesis of Variolin B and Deoxyvariolin B† , 2010 .

[282]  P. Kolkhof,et al.  Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists. , 2010, Bioorganic & medicinal chemistry letters.

[283]  S. Enthaler,et al.  Ammonia: an environmentally friendly nitrogen source for primary aniline synthesis. , 2010, ChemSusChem.

[284]  R. Grubbs,et al.  Synthesis and Structure of Fused N-Heterocylic Carbenes and Their Rhodium Complexes. , 2010, Organometallics.

[285]  I. Beletskaya,et al.  One‐Step Synthesis of Chiral Azamacrocycles via Palladium‐Catalyzed Enantioselective Amination of 1,5‐Dichloroanthraquinone and 1,5‐Dichloroanthracene , 2010 .

[286]  S. Buchwald,et al.  Palladium-Catalyzed Coupling of Functionalized Primary and Secondary Amines with Aryl and Heteroaryl Halides: Two Ligands Suffice in Most Cases. , 2010, Chemical science.

[287]  S. Buchwald,et al.  Dialkylbiaryl Phosphines in Pd-Catalyzed Amination: A User's Guide. , 2010, Chemical science.

[288]  L. Hardy,et al.  Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5. , 2010, Journal of medicinal chemistry.

[289]  S. Buchwald,et al.  Efficient Pd-catalyzed amination reactions for heterocycle functionalization. , 2010, Organic letters.

[290]  S. Buchwald,et al.  Palladium-catalyzed amination of unprotected halo-7-azaindoles. , 2010, Organic letters.

[291]  J. Peters,et al.  Ligand design for site-selective installation of Pd and Pt centers to generate homo- and heteropolymetallic motifs. , 2010, Chemical communications.

[292]  B. Maes,et al.  Synthesis of new tetracyclic azaheteroaromatic cores via auto-tandem Pd-catalyzed and one-pot Pd- and Cu-catalyzed double C-N bond formation , 2010 .

[293]  Yusheng Wu,et al.  Pd-catalyzed amidation of aryl(Het) halides with tert-butyl carbamate , 2010 .

[294]  I. Khanna,et al.  Facile, Regioselective Syntheses of N-Alkylated 2,3-Diaminopyridines and Imidazo(4,5-b)pyridines. , 2010 .

[295]  M. Willis,et al.  Palladium catalyzed tandem alkenyl- and aryl-C-N bond formation: a cascade N-annulation route to 4-, 5-, 6- and 7-chloroindoles , 2010 .

[296]  M. Lautens,et al.  The role of reversible oxidative addition in selective palladium(0)-catalyzed intramolecular cross-couplings of polyhalogenated substrates: synthesis of brominated indoles. , 2010, Journal of the American Chemical Society.

[297]  M. Ishikawa,et al.  Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. , 2010, Bioorganic & medicinal chemistry.

[298]  Michal M. Achmatowicz,et al.  Palladium‐Catalyzed Chemoselective Monoarylation of Hydrazides for the Synthesis of [1,2,4]Triazolo[4,3‐a]pyridines. , 2010 .

[299]  R. Roetz,et al.  2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression. , 2010, Bioorganic & medicinal chemistry letters.

[300]  F. Guengerich,et al.  The C8-2'-deoxyguanosine adduct of 2-amino-3-methylimidazo[1,2-d]naphthalene, a carbocyclic analogue of the potent mutagen 2-amino-3-methylimidazo[4,5-f]quinoline, is a block to replication in vitro. , 2010, Chemical research in toxicology.

[301]  Simon E. Hamilton,et al.  Process Development and Large-Scale Synthesis of a c-Met Kinase Inhibitor , 2010 .

[302]  M. Stradiotto,et al.  A P,N-ligand for palladium-catalyzed ammonia arylation: coupling of deactivated aryl chlorides, chemoselective arylations, and room temperature reactions. , 2010, Angewandte Chemie.

[303]  R. Batey,et al.  Substituted 2,5-diazabicyclo[4.1.0]heptanes and their application as general piperazine surrogates: synthesis and biological activity of a Ciprofloxacin analogue , 2010 .

[304]  Brian J. Kotecki,et al.  Synthesis of a TRPV1 Receptor Antagonist , 2010 .

[305]  S. Buchwald,et al.  Pd-catalyzed cross-coupling reactions of amides and aryl mesylates. , 2010, Organic letters.

[306]  P. Hergenrother,et al.  Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. , 2010, Journal of the American Chemical Society.

[307]  Steven V Ley,et al.  A flow-based synthesis of imatinib: the API of Gleevec. , 2010, Chemical communications.

[308]  S. Rault,et al.  Two-step synthesis of substituted 3-aminoindazoles from 2-bromobenzonitriles. , 2010, The Journal of organic chemistry.

[309]  Lutz Weber,et al.  On the industrial applications of MCRs: molecular diversity in drug discovery and generic drug synthesis , 2010, Molecular Diversity.

[310]  T. Hirano,et al.  Synthesis and properties of bis(pyrazino[2′,3′:4,5]imidazole)-fused 1,2,5,6-tetrahydro-1,4,5,8,9,10-hexaazaanthracenes: a new fluorescent nitrogen-rich heterocycle , 2010 .

[311]  J. Verkade,et al.  Highly Efficient Ligands for the Palladium‐Assisted Double N‐Arylation of Primary Amines for One‐Sep Construction of Carbazoles , 2010 .

[312]  Ed Cleator,et al.  A novel approach to 3-methylindoles by a Heck/cyclization/isomerization process. , 2010, Organic letters.

[313]  A. Verkman,et al.  Synthesis of a sensitive and selective potassium-sensing fluoroionophore. , 2010, Organic letters.

[314]  Peter M Fischer,et al.  Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5-dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors. , 2010, Journal of medicinal chemistry.

[315]  M. Stradiotto,et al.  A highly versatile catalyst system for the cross-coupling of aryl chlorides and amines. , 2010, Chemistry.

[316]  Xinquan Hu,et al.  Switching the chemoselectivity in the amination of 4-chloroquinazolines with aminopyrazoles. , 2010, Organic letters.

[317]  V. Young,et al.  Anionic amino acid [closo-1-CB9H8-1-COO-10-NH3]- and dinitrogen acid [closo-1-CB9H8-1-COOH-10-N2] as key precursors to advanced materials: synthesis and reactivity. , 2010, Inorganic chemistry.

[318]  C. Fleckenstein,et al.  Sterically demanding trialkylphosphines for palladium-catalyzed cross coupling reactions-alternatives to PtBu3. , 2010, Chemical Society reviews.

[319]  G. Bringmann,et al.  Total synthesis of the N,C-coupled naphthylisoquinoline alkaloids ancistrocladinium A and B and related analogues. , 2010, Journal of the American Chemical Society.

[320]  Michal M. Achmatowicz,et al.  Palladium-catalyzed chemoselective monoarylation of hydrazides for the synthesis of [1,2,4]triazolo[4,3-a]pyridines. , 2010, Organic letters.

[321]  Anna Wilhelmsson,et al.  1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists. , 2010, Bioorganic & medicinal chemistry letters.

[322]  Bin Xu,et al.  Palladium-catalyzed tandem amination reaction for the synthesis of 4-quinolones. , 2010, Organic letters.

[323]  M. Decker,et al.  Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors. , 2010, Journal of medicinal chemistry.

[324]  M. Beller,et al.  Recent Applications of Palladium‐Catalyzed Coupling Reactions in the Pharmaceutical, Agrochemical, and Fine Chemical Industries , 2009 .

[325]  D. Berger,et al.  Discovery of highly potent and selective type I B-Raf kinase inhibitors. , 2009, Bioorganic & medicinal chemistry letters.

[326]  S. Nolan,et al.  N-Heterocyclic Carbenes in Late Transition Metal Catalysis , 2009 .

[327]  I. Beletskaya,et al.  Palladium-Catalyzed Reactions of 4-(Trifluoromethylsulfonyloxy)coumarins with Amides and NH-Heterocycles , 2009 .

[328]  L. Adam,et al.  Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability. , 2009, Bioorganic & Medicinal Chemistry Letters.

[329]  S. Buchwald,et al.  Pd-catalyzed N-arylation of secondary acyclic amides: catalyst development, scope, and computational study. , 2009, Journal of the American Chemical Society.

[330]  Hui Xu Advances on N-Arylation of Indoles by Cross-Coupling Reactions , 2009 .

[331]  P. Guiry,et al.  New Thiazoline–Oxazoline Ligands and Their Application in the Asymmetric Friedel–Crafts Reaction , 2009 .

[332]  Yongwen Jiang,et al.  Assembly of substituted 1H-benzimidazoles and 1,3-dihydrobenzimidazol-2-ones via CuI/L-proline catalyzed coupling of aqueous ammonia with 2-iodoacetanilides and 2-iodophenylcarbamates. , 2009, The Journal of organic chemistry.

[333]  Jianhua Chao,et al.  Synthesis of functionalized hydroxy-thiophene motifs as amido- and sulfonamido-phenol bioisosteres , 2009 .

[334]  G. Cuny,et al.  One-Pot Synthesis of α-Carbolines via Sequential Palladium-Catalyzed Aryl Amination and Intramolecular Arylation. , 2009 .

[335]  M. Nazaré,et al.  A general and mild palladium-catalyzed domino reaction for the synthesis of 2H-indazoles. , 2009, Angewandte Chemie.

[336]  J. Hartwig,et al.  Palladium-catalyzed coupling of ammonia with aryl chlorides, bromides, iodides, and sulfonates: a general method for the preparation of primary arylamines. , 2009, Journal of the American Chemical Society.

[337]  P. T. Bremer,et al.  Rigid, Sterically Diverse N-Heterocyclic Carbene-Pyridine Chelates: Synthesis, Mild Palladation, and Palladium-Catalyzed Allylic Substitution , 2009 .

[338]  K. Hornberger,et al.  Mild Conditions for Pd‐Catalyzed Conversion of Aryl Bromides to Primary Anilines Using Benzophenone Imine. , 2009 .

[339]  Daoben Zhu,et al.  Heterocyclic annelated di(perylene bisimide): constructing bowl-shaped perylene bisimides by the combination of steric congestion and ring strain. , 2009, The Journal of organic chemistry.

[340]  S. Valiyaveettil,et al.  Synthesis and properties of symmetric and unsymmetric dibenzothienopyrroles. , 2009, Organic letters.

[341]  L. Neuville,et al.  Palladium-catalyzed domino N-arylation/carbopalladation/C-H functionalization: three-component synthesis of 3-(diarylmethylene)oxindoles , 2009 .

[342]  Laura G. Dubois,et al.  Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. , 2009, Journal of Medicinal Chemistry.

[343]  A. Waterson,et al.  Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate. , 2009, The Journal of organic chemistry.

[344]  S. Buchwald,et al.  An Efficient System For the Pd-Catalyzed Cross-Coupling of Amides and Aryl Chlorides. , 2009, Tetrahedron.

[345]  A. Börner,et al.  A general palladium-catalyzed amination of aryl halides with ammonia. , 2009, Chemistry.

[346]  M. Bröring,et al.  Bis-picket-fence corroles , 2009 .

[347]  M. Nishida,et al.  Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound , 2009, Proceedings of the National Academy of Sciences.

[348]  J. Jackson,et al.  Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. , 2009, Bioorganic & medicinal chemistry letters.

[349]  W. Erb,et al.  Ugi-post functionalization, from a single set of ugi-adducts to two distinct heterocycles by microwave-assisted palladium-catalyzed cyclizations: tuning the reaction pathways by ligand switch. , 2009, The Journal of organic chemistry.

[350]  D. Schollmeyer,et al.  First total synthesis of antiostatin A1, a potent carbazole-based naturally occurring antioxidant. , 2009, Chemical communications.

[351]  L. Djakovitch,et al.  Transition Metal‐Catalysed, Direct and Site‐Selective N1‐, C2‐ or C3‐Arylation of the Indole Nucleus: 20 Years of Improvements , 2009 .

[352]  K. Lawson,et al.  Synthesis of diazacalix[8]arene and triazacalix[12]arene methyl ethers via intramolecular aryl amination. , 2009, Organic letters.

[353]  S. Buchwald,et al.  A Highly Active Catalyst for Pd‐Catalyzed Amination Reactions: Cross‐Coupling Reactions Using Aryl Mesylates and the Highly Selective Monoarylation of Primary Amines Using Aryl Chlorides. , 2009 .

[354]  M. Cheung,et al.  Regioselective Synthesis of Benzimidazole Thiophene Inhibitors of Polo‐Like Kinase 1. , 2009 .

[355]  Jieping Zhu,et al.  Highly Enantioselective Aza Morita—Baylis—Hillman Reaction Catalyzed by Bifunctional β‐Isocupreidine Derivatives. , 2009 .

[356]  Brian J. Kotecki,et al.  A general method for the synthesis of unsymmetrically substituted ureas via palladium-catalyzed amidation. , 2009, Organic letters.

[357]  J. Bidlack,et al.  Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine. , 2009, Bioorganic & medicinal chemistry letters.

[358]  R. Andersen,et al.  Synthetic approaches to the microtubule-stabilizing sponge alkaloid ceratamine A and desbromo analogues. , 2009, The Journal of organic chemistry.

[359]  M. Willis,et al.  Cascade palladium-catalyzed alkenyl aminocarbonylation/ intramolecular aryl amidation: an annulative synthesis of 2-quinolones. , 2009, Organic letters.

[360]  D. M. Andrews,et al.  Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. , 2008, Bioorganic & medicinal chemistry letters.

[361]  V. Snieckus,et al.  Carbanionic Friedel-Crafts equivalents. regioselective directed ortho and remote metalation-C-N cross coupling routes to acridones and dibenzo[b,f]azepinones. , 2008, The Journal of organic chemistry.

[362]  Megerle L. Scherholz,et al.  Removal of Soluble Palladium Complexes from Reaction Mixtures by Fixed-Bed Adsorption , 2008 .

[363]  J. Hartwig Evolution of a fourth generation catalyst for the amination and thioetherification of aryl halides. , 2008, Accounts of chemical research.

[364]  Gitte Van Baelen,et al.  Synthesis of α‐Carbolines Starting from 2,3‐Dichloropyridines and Substituted Anilines , 2008 .

[365]  T. Ogata,et al.  Highly Reactive, General and Long-Lived Catalysts for Palladium-Catalyzed Amination of Heteroaryl and Aryl Chlorides, Bromides, and Iodides: Scope and Structure—Activity Relationships. , 2008 .

[366]  T. Ogata,et al.  Palladium-catalyzed amination of aryl and heteroaryl tosylates at room temperature. , 2008, Journal of the American Chemical Society.

[367]  J. Hartwig Carbon–heteroatom bond formation catalysed by organometallic complexes , 2008, Nature.

[368]  S. Nolan,et al.  Well-defined N-heterocyclic carbenes-palladium(II) precatalysts for cross-coupling reactions. , 2008, Accounts of chemical research.

[369]  Jieping Zhu,et al.  Highly enantioselective aza Morita-Baylis-Hillman reaction catalyzed by bifunctional beta-isocupreidine derivatives. , 2008, Journal of the American Chemical Society.

[370]  J. Hartwig,et al.  [(CyPF-(t)Bu)PdCl2]: an air-stable, one-component, highly efficient catalyst for amination of heteroaryl and aryl halides. , 2008, Organic letters.

[371]  W. Cheung,et al.  Discovery of piperidine carboxamide TRPV1 antagonists. , 2008, Bioorganic & medicinal chemistry letters.

[372]  S. Buchwald,et al.  Biaryl phosphane ligands in palladium-catalyzed amination. , 2008, Angewandte Chemie.

[373]  Xiao Mei Zheng,et al.  Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. , 2008, Bioorganic & Medicinal Chemistry Letters.

[374]  S. Hecht,et al.  Photoswitching of basicity. , 2008, Angewandte Chemie.

[375]  Y. Hashimoto,et al.  4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. , 2008, Bioorganic & medicinal chemistry.

[376]  P. Chou,et al.  Modulate photoinduced electron transfer efficiency of bipolar dendritic systems. , 2008, Organic letters.

[377]  D. Gelman,et al.  Trans-Spanned Palladium Catalyst for Mild and Efficient Amination of Aryl Halides with Benzophenone Imine. , 2008 .

[378]  K. Rex,et al.  Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). , 2008, Journal of Medicinal Chemistry.

[379]  M. Faul,et al.  A mild, one-pot synthesis of 4-quinolones via sequential Pd-catalyzed amidation and base-promoted cyclization. , 2008, Organic letters.

[380]  T. Ogata,et al.  Highly reactive, general and long-lived catalysts for palladium-catalyzed amination of heteroaryl and aryl chlorides, bromides, and iodides: scope and structure-activity relationships. , 2008, Journal of the American Chemical Society.

[381]  Sarah Luesse,et al.  A Preparation of enantiomerically enriched axially chiral beta-diketimines: synthesis of (-)- and (+)-IAN amine. , 2008, Organic letters.

[382]  N. Tohnai,et al.  Total synthesis of (-)-martinellic acid via radical addition-cyclization-elimination reaction. , 2008, The Journal of organic chemistry.

[383]  S. Whittaker,et al.  Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold. , 2008, Journal of medicinal chemistry.

[384]  S. Buchwald,et al.  A new class of easily activated palladium precatalysts for facile C-N cross-coupling reactions and the low temperature oxidative addition of aryl chlorides. , 2008, Journal of the American Chemical Society.

[385]  N. Chida,et al.  Total synthesis of (+/-)-murrayazoline. , 2008, Organic letters.

[386]  R. Batey,et al.  Copper-catalyzed domino annulation approaches to the synthesis of benzoxazoles under microwave-accelerated and conventional thermal conditions. , 2008, The Journal of organic chemistry.

[387]  V. Lynch,et al.  Diaminocarbene[3]ferrocenophanes and their transition-metal complexes. , 2008, Angewandte Chemie.

[388]  Hong Zhu,et al.  Development of prodrug 4-chloro-3-(5-methyl-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}-1,2,4-benzotriazin-7-yl)phenyl benzoate (TG100801): a topically administered therapeutic candidate in clinical trials for the treatment of age-related macular degeneration. , 2008, Journal of medicinal chemistry.

[389]  Alberto Coelho,et al.  Auto-Tandem Catalysis : Synthesis of Substituted 11H-Indolo [3,2-c]quinolines via Palladium-Catalyzed Intermolecular C-N and Intramolecular C-C Bond Formation , 2008 .

[390]  K. Nozaki,et al.  Synthesis, structures, and properties of unsymmetrical heteroacenes containing both pyrrole and furan rings. , 2008, Organic letters.

[391]  P. Nielsen,et al.  Palladium-catalyzed three-component approach to promazine with formation of one carbon-sulfur and two carbon-nitrogen bonds. , 2008, Angewandte Chemie.

[392]  Mohammed M. Abadleh,et al.  Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors. , 2008, Bioorganic & medicinal chemistry letters.

[393]  C. Bertozzi,et al.  Synthetic studies toward Mycobacterium tuberculosis sulfolipid-I. , 2008, The Journal of organic chemistry.

[394]  B. Bang-Andersen,et al.  Palladium-catalyzed aryl amination-heck cyclization cascade: a one-flask approach to 3-substituted indoles. , 2008, Angewandte Chemie.

[395]  R. Nilakantan,et al.  Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90. , 2008, Journal of medicinal chemistry.

[396]  H. Tsou,et al.  Palladium-catalyzed arylation of N,N-dialkylhydrazines and the subsequent conversion to anilines , 2007 .

[397]  S. Buchwald,et al.  Copper-catalyzed regiospecific synthesis of N-alkylbenzimidazoles. , 2007, Organic letters.

[398]  M. Lang,et al.  Applicability Aspects of Transition Metal‐Catalyzed Aromatic Amination Protocols in Medicinal Chemistry , 2007 .

[399]  S. Buchwald,et al.  Pd-catalyzed amidation of aryl chlorides using monodentate biaryl phosphine ligands: a kinetic, computational, and synthetic investigation. , 2007, Journal of the American Chemical Society.

[400]  S. Buchwald,et al.  A palladium-catalyzed regiospecific synthesis of N-aryl benzimidazoles. , 2007, Angewandte Chemie.

[401]  J. A. Vega,et al.  Fluorous-tagged carbamates for the pd-catalyzed amination of aryl halides. , 2007, The Journal of organic chemistry.

[402]  S. Buchwald,et al.  Selective palladium-catalyzed arylation of ammonia: synthesis of anilines as well as symmetrical and unsymmetrical di- and triarylamines. , 2007, Journal of the American Chemical Society.

[403]  Alison R. Gregro,et al.  Discovery of Isonicotinamide Derived β-Secretase Inhibitors: In Vivo Reduction of β-Amyloid , 2007 .

[404]  V. Gevorgyan,et al.  Direct transition metal-catalyzed functionalization of heteroaromatic compounds. , 2007, Chemical Society reviews.

[405]  A. Mortlock,et al.  Two New Syntheses of a 4-Aminopyrazole: Condensation of an N-Substituted Vinamidinium Salt with a Functionalized Hydrazine , 2007 .

[406]  R. Wilkes,et al.  Highly Functionalised Sulfur-Based Silica Scavengers for the Efficient Removal of Palladium Species from Active Pharmaceutical Ingredients , 2007 .

[407]  M. Organ,et al.  Palladium complexes of N-heterocyclic carbenes as catalysts for cross-coupling reactions--a synthetic chemist's perspective. , 2007, Angewandte Chemie.

[408]  D. Ma,et al.  Synthesis of 1,2-disubstituted benzimidazoles by a Cu-catalyzed cascade aryl amination/condensation process. , 2007, Angewandte Chemie.

[409]  L. Ackermann,et al.  Domino N-H/C-H bond activation: palladium-catalyzed synthesis of annulated heterocycles using dichloro(hetero)arenes. , 2007, Angewandte Chemie.

[410]  G. Fabrizi,et al.  Palladium‐Catalyzed N‐Arylation of N,N‐Dialkylhydrazines with Aryl Chlorides , 2007 .

[411]  M. Kerr,et al.  Aryl amidation routes to dihydropyrrolo[3,2-e]indoles and pyrrolo[3,2-f]tetrahydroquinolines: total synthesis of the (+/-)-CC-1065 CPI subunit. , 2007, The Journal of organic chemistry.

[412]  Thomas M. Razler,et al.  Inhibitors of unactivated p38 MAP kinase. , 2006, Bioorganic & medicinal chemistry letters.

[413]  R. Bedford,et al.  N-H carbazole synthesis from 2-chloroanilines via consecutive amination and C-H activation. , 2006, The Journal of organic chemistry.

[414]  S. Buchwald,et al.  Monodentate phosphines provide highly active catalysts for Pd-catalyzed C-N bond-forming reactions of heteroaromatic halides/amines and (H)N-heterocycles. , 2006, Angewandte Chemie.

[415]  M. Willis,et al.  Tandem palladium-catalyzed urea arylation-intramolecular ester amidation: regioselective synthesis of 3-alkylated 2,4-quinazolinediones. , 2006, Organic letters.

[416]  Jieping Zhu,et al.  Rapid access to oxindoles by the combined use of an Ugi four-component reaction and a microwave-assisted intramolecular Buchwald-Hartwig amidation reaction. , 2006, Organic letters.

[417]  Noritaka Chida,et al.  One-step construction of carbazoles by way of the palladium-catalyzed double N-arylation reaction and its application to the total synthesis of murrastifoline-A , 2006 .

[418]  J. Hartwig,et al.  Palladium-catalyzed coupling of ammonia and lithium amide with aryl halides. , 2006, Journal of the American Chemical Society.

[419]  M. Teulade‐Fichou,et al.  Improved Synthesis of Quinacridine Derivatives. , 2006 .

[420]  G. Mignani,et al.  Selected patented cross-coupling reaction technologies. , 2006, Chemical reviews.

[421]  M. Yamashita,et al.  Organometallic chemistry of amidate complexes. accelerating effect of bidentate ligands on the reductive elimination of N-aryl amidates from palladium(II). , 2006, Journal of the American Chemical Society.

[422]  I. Davies,et al.  Efficient access to cyclic ureas via Pd-catalyzed cyclization. , 2006, Organic letters.

[423]  J. S. Carey,et al.  Analysis of the reactions used for the preparation of drug candidate molecules. , 2006, Organic & biomolecular chemistry.

[424]  Nicolas Marion,et al.  (IPr)Pd(acac)Cl: an easily synthesized, efficient, and versatile precatalyst for C-N and C-C bond formation. , 2006, The Journal of organic chemistry.

[425]  B. Maes,et al.  Orthogonal and auto-tandem catalysis: synthesis of dipyrido[1,2-a:2',3'-d]imidazole and its benzo and aza analogues via inter- and intramolecular C-N bond formation. , 2006, The Journal of organic chemistry.

[426]  S. Buchwald,et al.  Expedited palladium-catalyzed amination of aryl nonaflates through the use of microwave-irradiation and soluble organic amine bases. , 2006, The Journal of organic chemistry.

[427]  C. Vilanova,et al.  Regioselective Preparation of Pyridin‐2‐yl Ureas from 2‐Chloropyridines Catalyzed by Pd(0). , 2005 .

[428]  D. Fichou,et al.  Triazatrinaphthylene, a three-fold symmetry planar conjugated system with two-dimensional self-assembly properties , 2005 .

[429]  G. Mignani,et al.  The Synthesis of Important Pharmaceutical Building Blocks by Palladium‐Catalyzed Coupling Reaction: Access to Various Arylhydrazines , 2005 .

[430]  W. Xiao,et al.  Base effect and inhibition of catalytic activity in palladium-catalyzed N-heteroarylation of pyrazoles with 2,6-dibromopyridine , 2005 .

[431]  Louis-Charles Campeau,et al.  High-yielding intramolecular direct arylation reactions with aryl chlorides. , 2005, Organic letters.

[432]  G. Fabrizi,et al.  Synthesis of N,N-Dialkyl-N'-arylhydrazines via palladium-catalyzed N-arylation by using N,N-dialkylhydrazines/2LiCl adducts. , 2005, Organic letters.

[433]  J. Hartwig,et al.  Zinc trimethylsilylamide as a mild ammonia equivalent and base for the amination of aryl halides and triflates. , 2005, Organic letters.

[434]  S. Shekhar,et al.  Highly reactive, general, and long-lived catalysts for coupling heteroaryl and aryl chlorides with primary nitrogen nucleophiles. , 2005, Angewandte Chemie.

[435]  A. Kuwahara,et al.  Double N-arylation of primary amines: carbazole synthesis from 2,2'-biphenyldiols. , 2005, The Journal of organic chemistry.

[436]  M. Willis,et al.  Palladium-catalyzed tandem alkenyl and aryl C--N bond formation: a cascade N-annulation route to 1-functionalized indoles. , 2005, Angewandte Chemie.

[437]  U. Scholz,et al.  Palladium‐Catalyzed CN and CO Coupling–A Practical Guide from an Industrial Vantage Point† , 2004 .

[438]  M. Nieger,et al.  Sulfamide Synthesis via Pd-Catalysed Cross-Coupling , 2004 .

[439]  R. Dommisse,et al.  The first tandem double palladium-catalyzed aminations: synthesis of dipyrido[1,2-a:3',2'-d]imidazole and its benzo- and aza-analogues. , 2004, Chemical communications.

[440]  K. B. Fields,et al.  Bromoporphyrins as versatile synthons for modular construction of chiral porphyrins: cobalt-catalyzed highly enantioselective and diastereoselective cyclopropanation. , 2004, Journal of the American Chemical Society.

[441]  G. Mignani,et al.  An Efficient and Safe Procedure for the Large-Scale Pd-Catalyzed Hydrazonation of Aromatic Chlorides Using Buchwald Technology , 2004 .

[442]  R. J. Herr,et al.  Convenient Palladium‐Catalyzed Preparation of Primary Anilines Using a Fluorous Benzophenone Imine Reagent. , 2004 .

[443]  P. Guiry,et al.  Recent developments in the application of oxazoline-containing ligands in asymmetric catalysis. , 2004, Chemical reviews.

[444]  L. Alcaraz,et al.  Novel N-aryl and N-heteroaryl sulfamide synthesis via palladium cross coupling. , 2004, Organic letters.

[445]  Q. Guo,et al.  Amino Acid Mediated Goldberg Reactions Between Amides and Aryl Iodides. , 2004 .

[446]  X. Zhang,et al.  General synthesis of meso-amidoporphyrins via palladium-catalyzed amidation. , 2004, Organic letters.

[447]  G. Burton,et al.  Palladium-catalyzed intermolecular coupling of aryl chlorides and sulfonamides under microwave irradiation. , 2003, Organic letters.

[448]  A. Szymańska,et al.  Synthesis of N-[(tert-Butoxy)carbonyl]-3-(9,10-dihydro-9-oxoacridin-2-yl)-L-alanine, a New Fluorescent Amino Acid Derivative , 2003 .

[449]  C. Brain,et al.  An improved procedure for the synthesis of benzimidazoles, using palladium-catalyzed aryl-amination chemistry. , 2003, The Journal of organic chemistry.

[450]  J. Hartwig,et al.  Understanding the coupling of heteroaromatic substrates: Synthesis, structures, and reductive eliminations of heteroarylpalladium amido complexes , 2003 .

[451]  I. Beletskaya,et al.  Variation of xanthene-based bidentate ligands in the palladium-catalyzed arylation of ureas , 2003 .

[452]  S. Buchwald,et al.  An air and thermally stable one- component catalyst for the amination of aryl chlorides. , 2003, Organic letters.

[453]  Arun K. Ghosh,et al.  Palladium-catalyzed synthesis of N-aryloxazolidinones from aryl chlorides. , 2003, Organic letters.

[454]  T. Hiyama,et al.  The double N-arylation of primary amines: toward multisubstituted carbazoles with unique optical properties. , 2003, Angewandte Chemie.

[455]  S. Buchwald,et al.  Expanding Pd-catalyzed C-N bond-forming processes: the first amidation of aryl sulfonates, aqueous amination, and complementarity with Cu-catalyzed reactions. , 2003, Journal of the American Chemical Society.

[456]  J. Hartwig,et al.  Scope and mechanism of palladium-catalyzed amination of five-membered heterocyclic halides. , 2003, The Journal of organic chemistry.

[457]  C. Cho,et al.  Novel route to azobenzenes via Pd-catalyzed coupling reactions of aryl hydrazides with aryl halides, followed by direct oxidations. , 2003, Organic letters.

[458]  R. Batey,et al.  Copper- and palladium-catalyzed intramolecular aryl guanidinylation: an efficient method for the synthesis of 2-aminobenzimidazoles. , 2003, Organic letters.

[459]  P. Guiry,et al.  Coupling of bulky, electron-deficient partners in aryl amination in the preparation of tridentate bis(oxazoline) ligands for asymmetric catalysis. , 2002, The Journal of organic chemistry.

[460]  O. Schärer,et al.  Preparation of C8-amine and acetylamine adducts of 2'-deoxyguanosine suitably protected for DNA synthesis. , 2002, Organic letters.

[461]  A. Schnyder,et al.  A new generation of air stable, highly active Pd complexes for C--C and C--N coupling reactions with aryl chlorides. , 2002, Angewandte Chemie.

[462]  M. Huffman,et al.  Pd-catalyzed N-arylation of heteroarylamines. , 2002, Organic letters.

[463]  M. Lakshman Palladium-catalyzed C–N and C–C cross-couplings as versatile, new avenues for modifications of purine 2′-deoxynucleosides , 2002 .

[464]  D. Boykin,et al.  Palladium-catalyzed N-arylation of O-methylamidoximes , 2002 .

[465]  S. Buchwald,et al.  Pd-catalyzed intermolecular amidation of aryl halides: the discovery that xantphos can be trans-chelating in a palladium complex. , 2002, Journal of the American Chemical Society.

[466]  C. Brain,et al.  An intramolecular palladium-catalysed aryl amination reaction to produce benzimidazoles , 2002 .

[467]  S. Nolan,et al.  Amination reactions of aryl halides with nitrogen-containing reagents mediated by palladium/imidazolium salt systems. , 2001, The Journal of organic chemistry.

[468]  S. Buchwald,et al.  New ammonia equivalents for the Pd-catalyzed amination of aryl halides. , 2001, Organic letters.

[469]  J. Hartwig,et al.  Palladium-catalyzed synthesis of arylamines from aryl halides and lithium bis(trimethylsilyl)amide as an ammonia equivalent. , 2001, Organic letters.

[470]  I. Beletskaya,et al.  Palladium-catalyzed reaction of aryl halides with ureas , 2001 .

[471]  P. Seeberger,et al.  Halobenzyl Ethers as Protecting Groups for Organic Synthesis , 2000 .

[472]  S. Buchwald,et al.  Efficient palladium-catalyzed N-arylation of indoles. , 2000, Organic letters.

[473]  S. Buchwald,et al.  Palladium-catalyzed intermolecular coupling of aryl halides and amides. , 2000, Organic letters.

[474]  S. Buchwald,et al.  Simple, efficient catalyst system for the palladium-catalyzed amination of aryl chlorides, bromides, and triflates. , 2000, The Journal of organic chemistry.

[475]  S. Buchwald,et al.  Scope and limitations of the Pd/BINAP-catalyzed amination of aryl bromides. , 2000, The Journal of organic chemistry.

[476]  Stephen L. Buchwald,et al.  A Palladium-Catalyzed Method for the Preparation of Indoles via the Fischer Indole Synthesis , 1999 .

[477]  J. Hartwig,et al.  Room-Temperature Palladium-Catalyzed Amination of Aryl Bromides and Chlorides and Extended Scope of Aromatic C-N Bond Formation with a Commercial Ligand. , 1999, The Journal of organic chemistry.

[478]  S. Buchwald,et al.  The development of efficient protocols for the palladium-catalyzed cyclization reactions of secondary amides and carbamates. , 1999, Organic letters.

[479]  G. Bridger,et al.  Regioselective synthesis of aryl hydrazides by palladium-catalyzed coupling of t-butylcarbazate with substituted aryl bromides , 1999 .

[480]  S. Buchwald,et al.  Rational Development of Practical Catalysts for Aromatic Carbon—Nitrogen Bond Formation , 1999 .

[481]  J. Hartwig Transition Metal Catalyzed Synthesis of Arylamines and Aryl Ethers from Aryl Halides and Triflates: Scope and Mechanism. , 1998, Angewandte Chemie.

[482]  J. Hartwig Synthesis, Structure, and Reactivity of a Palladium Hydrazonato Complex: A New Type of Reductive Elimination Reaction To Form C-N Bonds and Catalytic Arylation of Benzophenone Hydrazone. , 1998, Angewandte Chemie.

[483]  S. Buchwald,et al.  A Palladium-Catalyzed Strategy for the Preparation of Indoles: A Novel Entry into the Fischer Indole Synthesis , 1998 .

[484]  Yamamoto Toshihide,et al.  Palladium-catalyzed synthesis of triarylamines from aryl halides and diarylamines , 1998 .

[485]  J. Hartwig,et al.  Palladium-Catalyzed C−N(sp2) Bond Formation: N-Arylation of Aromatic and Unsaturated Nitrogen and the Reductive Elimination Chemistry of Palladium Azolyl and Methyleneamido Complexes , 1998 .

[486]  S. Buchwald,et al.  An Ammonia Equivalent for the Palladium-Catalyzed Amination of Aryl Halides and Triflates , 1997 .

[487]  S. Buchwald,et al.  Intramolecular palladium-catalyzed aryl amination and aryl amidation , 1996 .

[488]  M. Beller,et al.  Palladacycles as Structurally Defined Catalysts for the Heck Olefination of Chloro- and Bromoarenes†‡ , 1995 .

[489]  I. Khanna,et al.  Facile, Regioselective Syntheses of N-Alkylated 2,3-Diaminopyridines and Imidazo[4,5-b]pyridines , 1995 .

[490]  K. Carlin,et al.  N-Aryl azacycles as novel sodium channel blockers. , 2015, Bioorganic & medicinal chemistry letters.

[491]  姚长江,et al.  Strongly coupled cyclometalated ruthenium–triarylamine hybrids: tuning electrochemical properties, intervalence charge transfer, and spin distribution by substituent effects , 2014 .

[492]  M. Nazaré,et al.  A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines , 2011 .

[493]  R. Schreiber,et al.  Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor. , 2011, Bioorganic & medicinal chemistry letters.

[494]  J. I. van der Vlugt Advances in selective activation and application of ammonia in homogeneous catalysis. , 2010, Chemical Society reviews.

[495]  M. Funk,et al.  Investigating different strategies towards the preparation of chiral and achiral bis-picket fence corroles , 2009 .

[496]  J. Kámán,et al.  Syntheses of new quinoline‐containing heterocyclic scaffolds using inter‐ and intramolecular Pd‐catalyzed amination , 2009 .

[497]  S. Buchwald,et al.  Industrial-Scale Palladium-Catalyzed Coupling of Aryl Halides and Amines –A Personal Account , 2006 .

[498]  T. Sakamoto,et al.  Novel synthetic strategy of carbolines via palladium-catalyzed amination and arylation reaction , 1999 .