Jinhua J. Song

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Best Practices for Drug Substance Stress and Stability Studies During Early Stage Development. Part III—How to Make Science- and Risk-based Stability Testing Decisions for Drug Substance Batches Produced after Manufacturing Process Changes

Fenghe Qiu, Q. Chan Li, Will McWilliams, 2013, Journal of Pharmaceutical Innovation.

Best Practices for Drug Substance Stress and Stability Studies During Early-Stage Development Part I—Conducting Drug Substance Solid Stress to Support Phase Ia Clinical Trials

Jinhua J. Song, Q. Chan Li, F. Qiu, 2012, Journal of Pharmaceutical Innovation.

The Eight Criteria Defining a Good Chemical Manufacturing Process

Rolf Dach, Frank Roschangar, Jinhua J. Song, 2012 .

Activation of TMSCN by N-heterocyclic carbenes for facile cyanosilylation of carbonyl compounds.

Jinhua J. Song, C. Senanayake, F. Gallou, 2006, The Journal of organic chemistry.

Preparative Synthesis via Continuous Flow of 4,4,5,5-Tetramethyl-2-(3-trimethylsilyl-2-propynyl)-1,3,2-dioxaborolane: A General Propargylation Reagent

Jinhua J. Song, C. Senanayake, J. T. Reeves, 2012 .

The Growing Impact of Catalysis in the Pharmaceutical Industry

Jinhua J. Song, Chris H. Senanayake, C. Senanayake, 2011 .

Development of a large scale asymmetric synthesis of the glucocorticoid agonist BI 653048 BS H3PO4.

Jinhua J. Song, B. Narayanan, C. Senanayake, 2013, The Journal of organic chemistry.

9.3 Industrial Applications of Asymmetric Synthesis: Asymmetric Synthesis as an Enabler of Green Chemistry

Jinhua J. Song, C. Senanayake, D. Krishnamurthy, 2012 .

Development of a Safe and Economical Synthesis of Methyl 6-Chloro-5-(trifluoromethyl)nicotinate: Trifluoromethylation on Kilogram Scale

Jinhua J. Song, C. Senanayake, J. Mulder, 2013 .

Sequential C-H Arylation and Enantioselective Hydrogenation Enables Ideal Asymmetric Entry to the Indenopiperidine Core of an 11β-HSD-1 Inhibitor.

Jinhua J. Song, Bing-Shiou Yang, Jun Wang, 2016, Journal of the American Chemical Society.

Reengineered BI-DIME Ligand Core Based on Computer Modeling to Increase Selectivity in Asymmetric Suzuki–Miyaura Coupling for the Challenging Axially Chiral HIV Integrase Inhibitor

Jinhua J. Song, C. Senanayake, N. Yee, 2016 .

Synthesis of Enantioenriched 2-Alkyl Piperidine Derivatives through Asymmetric Reduction of Pyridinium Salts.

Jinhua J. Song, C. Senanayake, Xudong Wei, 2016, Organic letters.

Synthesis of P-Chiral Dihydrobenzooxaphospholes Through Negishi Cross-Coupling.

Jinhua J. Song, C. Senanayake, N. Yee, 2016, The Journal of organic chemistry.

Large Scale Practical Synthesis of Enantiomerically Pure cis-4-Amino-3-fluoro-1-methylpiperidine via Rhodium-Catalyzed Asymmetric Hydrogenation of a Tetrasubstituted Fluoroalkene

Jinhua J. Song, C. Senanayake, Heewon Lee, 2021 .

Synthesis of p38 MAP kinase inhibitor BIRB 796 and analogs via copper-mediated N-arylation reaction

Jinhua J. Song, N. Yee, Daniel R Fandrick, 2010 .

Asymmetric methallylation of ketones catalyzed by a highly active organocatalyst 3,3'-F2-BINOL.

Jinhua J. Song, Jun Wang, C. Senanayake, 2013, Organic letters.

Transition Metal Catalysis in the Pharmaceutical Industry

Jinhua J. Song, C. Senanayake, Daniel R Fandrick, 2012 .

Efficient Iron‐Catalyzed Kumada Cross‐Coupling Reactions Utilizing Flow Technology under Low Catalyst Loadings

Jinhua J. Song, Bing-Shiou Yang, C. Senanayake, 2016 .

Synthesis of C1C8 and C9C24 fragments of (−)-discodermolide: use of asymmetric alkylation and stereoselective aldol reactions☆

Jinhua J. Song, S. Masamune, S. Filla, 1999 .

Copper-catalyzed asymmetric hydrogenation of 2-substituted ketones via dynamic kinetic resolution† †Electronic supplementary information (ESI) available. CCDC 1816601 and 1816602. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c8sc00434j

Joyce C. Leung, Jinhua J. Song, C. Senanayake, 2018, Chemical science.

Copper catalyzed asymmetric propargylation of aldehydes.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, Journal of the American Chemical Society.

Development of an asymmetric synthesis of a chiral quaternary FLAP inhibitor.

Jinhua J. Song, C. Senanayake, P. Mahaney, 2015, The Journal of organic chemistry.

Synthesis of empagliflozin, a novel and selective sodium-glucose co-transporter-2 inhibitor, labeled with carbon-14 and carbon-13.

Jinhua J. Song, C. Senanayake, Heewon Lee, 2014, Journal of labelled compounds & radiopharmaceuticals.

Zinc catalyzed and mediated propargylations with propargyl boronates.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, Organic letters.

Zinc catalyzed and mediated asymmetric propargylation of trifluoromethyl ketones with a propargyl boronate.

Jinhua J. Song, B. Narayanan, C. Senanayake, 2013, The Journal of organic chemistry.

Early Development Scale-Up of a Structurally-Challenging 5-Lipoxygenase Activating Protein (FLAP) Inhibitor

Jinhua J. Song, Jun Wang, C. Senanayake, 2017 .

Remarkable enhancement of enantioselectivity in the asymmetric conjugate addition of dimethylzinc to (Z)-nitroalkenes with a catalytic [(MeCN)₄Cu]PF₆-Hoveyda ligand complex.

Jinhua J. Song, C. Senanayake, J. Mulder, 2014, Angewandte Chemie.

Achieving synthetic efficiency through new method development

Jinhua J. Song, C. Senanayake, N. Yee, 2008 .

Process Development of the BACE Inhibitors BI 1147560 BS and BI 1181181 MZ

Jinhua J. Song, S. Venkatraman, C. Senanayake, 2022, Organic Process Research & Development.

Zinc-catalyzed allenylations of aldehydes and ketones.

Jinhua J. Song, C. Senanayake, K. Fandrick, 2011, Organic letters.

Organometallic methods for the synthesis and functionalization of azaindoles.

Fabrice Gallou, Jinhua J. Song, C. Senanayake, 2007, Chemical Society reviews.

Development of an Efficient Asymmetric Synthesis of the Chiral Quaternary 5-Lipoxygenase Activating Protein Inhibitor

Jinhua J. Song, C. Senanayake, J. Mulder, 2016 .

Development of an Asymmetric Route for Large-Scale Synthesis of a Glucocorticoid Agonist

Jinhua J. Song, Bing-Shiou Yang, C. Senanayake, 2016 .

One-step construction of 2-substituted-4,6-diazaindoles from carboxylic acid derivatives

Jinhua J. Song, C. Senanayake, N. Yee, 2009 .

Practical regioselective bromination of azaindoles and diazaindoles

Jinhua J. Song, C. Senanayake, F. Gallou, 2007 .

Regioselective halogenation of 6-azaindoles : Efficient synthesis of 3-halo-2,3-disubstituted-6-azaindole derivatives

Jinhua J. Song, C. Senanayake, F. Gallou, 2005 .

A novel one-step synthesis of 2-substituted 6-azaindoles from 3-amino-4-picoline and carboxylic esters.

Jinghua Xu, Fabrice Gallou, Jinhua J. Song, 2005, The Journal of organic chemistry.

Development of a Practical Sequence for Difluoromethylation of 2‐Bromopyridines via Copper‐Mediated Reductive Coupling and Decarboxylation

Jinhua J. Song, C. Senanayake, Xudong Wei, 2015 .

DielsAlder Cyclization of a Dihydropyridine: NMR Spectroscopy, X‐Ray Crystallography, and DFT Computations. Bent Aromatic Dimeric Clusters in the Solid Phase

Jinhua J. Song, J. Gallucci, G. Fraenkel, 2014 .

A One-Pot Organometallic Route from a 4-Alkenylpyridine to a 4,4-Spiro-Linked Ethyl 1,4-Dihydropyridine-1-carboxylate

Jinhua J. Song, J. Gallucci, G. Fraenkel, 2012 .

Synthesis of 1-aryl-1 H -indazoles via the palladium-catalyzed cyclization of N -aryl- N ′-( o -bromobenzyl)hydrazines and [ N -aryl- N ′-( o -bromobenzyl)-hydrazinato- N ′]-triphenylphosphonium bromides

Jinhua J. Song, N. Yee, 2001 .

N-heterocyclic carbene-catalyzed silyl enol ether formation.

Jinhua J. Song, C. Senanayake, N. Yee, 2008, Organic letters.

N-heterocyclic carbene-catalyzed Mukaiyama aldol reactions.

Jinhua J. Song, C. Senanayake, N. Yee, 2007, Organic letters.

Challenges and Opportunities for Scaling the Ring‐Closing Metathesis Reaction in the Pharmaceutical Industry

Jinhua J. Song, C. Senanayake, N. Yee, 2014 .

Development of an Enantioselective Hydrogenation Route to (S)-1-(2-(Methylsulfonyl)pyridin-4-yl)propan-1-amine

Jinhua J. Song, Bing-Shiou Yang, C. Senanayake, 2014 .

Large-Scale Enantioselective Reduction of 2,3-Disubstituted Indenopyridine Enables a Practical Manufacturing Process for an 11β-HSD-1 Inhibitor

Jinhua J. Song, Bing-Shiou Yang, Jun Wang, 2021, Organic Process Research & Development.

Enantioselective Synthesis of α-(Hetero)aryl Piperidines through Asymmetric Hydrogenation of Pyridinium Salts and Its Mechanistic Insights.

Jinhua J. Song, C. Senanayake, M. Kozlowski, 2018, Organic letters.

Copper-catalyzed annulation of 2-formylazoles with o-aminoiodoarenes.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, The Journal of organic chemistry.

A mild dihydrobenzooxaphosphole oxazoline/iridium catalytic system for asymmetric hydrogenation of unfunctionalized dialins.

Jinhua J. Song, C. Senanayake, K. McKellop, 2014, Angewandte Chemie.

Synthesis of pyridyl-dihydrobenzooxaphosphole ligands and their application in asymmetric hydrogenation of unfunctionalized alkenes.

Jinhua J. Song, C. Senanayake, Xudong Wei, 2014, The Journal of organic chemistry.

A versatile catalyst system for enantioselective synthesis of 2-substituted 1,4-benzodioxanes† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c8sc05612a

Joyce C. Leung, Jinhua J. Song, C. Senanayake, 2019, Chemical science.

Computationally Assisted Mechanistic Investigation and Development of Pd-Catalyzed Asymmetric Suzuki-Miyaura and Negishi Cross-Coupling Reactions for Tetra-ortho-Substituted Biaryl Synthesis.

Jinhua J. Song, C. Senanayake, M. Kozlowski, 2018, ACS catalysis.

Hepatitis C virus serine protease: synthesis of radioactive and stable isotope-labeled potent inhibitors.

Jinhua J. Song, C. Senanayake, V. Gorys, 2014, Journal of labelled compounds & radiopharmaceuticals.

Development of a Large-Scale Asymmetric Process for tert-Butanesulfinamide

Jinhua J. Song, C. Senanayake, Heewon Lee, 2019, Organic Process Research & Development.

Application of a Preformed Pd-BIDIME Precatalyst to Suzuki-Miyaura Cross-Coupling Reaction in Flow.

Jinhua J. Song, C. Senanayake, N. Yee, 2019, The Journal of organic chemistry.

General and rapid pyrimidine condensation by addressing the rate limiting aromatization.

Jinhua J. Song, C. Senanayake, K. Fandrick, 2014, Organic letters.

Asymmetric synthesis of active pharmaceutical ingredients.

Jinhua J. Song, C. Senanayake, Vittorio Farina, 2006, Chemical reviews.

N-heterocyclic carbene-catalyzed Mukaiyama aldol reactions.

Jinhua J. Song, C. Senanayake, N. Yee, 2007, Organic letters.

Highly diastereoselective zinc-catalyzed propargylation of tert-butanesulfinyl imines.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, Organic letters.

Regioselective allene synthesis and propargylations with propargyl diethanolamine boronates.

Jinhua J. Song, C. Senanayake, N. Yee, 2009, Organic letters.

Efficient asymmetric synthesis of P-chiral phosphine oxides via properly designed and activated benzoxazaphosphinine-2-oxide agents.

Jinhua J. Song, C. Senanayake, Shengli Ma, 2013, Journal of the American Chemical Society.

Efficient asymmetric synthesis of structurally diverse P-stereogenic phosphinamides for catalyst design.

Jinhua J. Song, C. Senanayake, N. Yee, 2015, Angewandte Chemie.

Development of new P-chiral P,π-dihydrobenzooxaphosphole hybrid ligands for asymmetric catalysis.

Jinhua J. Song, C. Senanayake, K. Fandrick, 2014, Organic letters.

General and Stereoselective Method for the Synthesis of Sterically Congested and Structurally Diverse P-Stereogenic Secondary Phosphine Oxides.

Jinhua J. Song, C. Senanayake, K. Fandrick, 2017, Organic letters.

Development of a Scalable, Chromatography-Free Synthesis of t-Bu-SMS-Phos and Application to the Synthesis of an Important Chiral CF3-Alcohol Derivative with High Enantioselectivity Using Rh-Catalyzed Asymmetric Hydrogenation.

Jinhua J. Song, B. Narayanan, C. Senanayake, 2018, The Journal of organic chemistry.

P‐Stereogenic Chiral Phosphine−Palladium Complex Catalyzed Enantioselective Synthesis of Phosphoryl‐Substituted Atropisomeric Vinylarenes

Jinhua J. Song, C. Senanayake, Heewon Lee, 2017 .

Development of a Practical Synthesis of 4-[6-(Morpholinomethyl)-pyridin-3-yl]naphthalen-1-amine, a Key Intermediate for the Synthesis of BIRB 1017, a Potent p38 MAP Kinase Inhibitor

Jinhua J. Song, C. Senanayake, N. Yee, 2013 .

Development of a concise, scalable synthesis of a CCR1 antagonist utilizing a continuous flow Curtius rearrangement

Jinhua J. Song, B. Narayanan, Bing-Shiou Yang, 2017 .

Enantioselective Nickel-Catalyzed Mizoroki-Heck Cyclizations To Generate Quaternary Stereocenters.

Jinhua J. Song, C. Senanayake, M. Kozlowski, 2017, Organic letters.

Copper‐Catalyzed Annulation of 2‐Formylazoles with o‐Aminoiodoarenes.

Jinhua J. Song, C. Senanayake, N. Yee, 2010 .

Design and synthesis of chiral oxathiozinone scaffolds: efficient synthesis of hindered enantiopure sulfinamides and sulfinyl ketimines.

Jinhua J. Song, C. Senanayake, Shengli Ma, 2013, Angewandte Chemie.

Facile entry to an efficient and practical enantioselective synthesis of a polycyclic cholesteryl ester transfer protein inhibitor.

Jinhua J. Song, M. Ostermeier, J. Mack, 2014, Organic letters.

Mild and general zinc-alkoxide-catalyzed allylations of ketones with allyl pinacol boronates.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, Organic letters.

Addressing the configuration stability of lithiated secondary benzylic carbamates for the development of a noncryogenic stereospecific boronate rearrangement.

Jinhua J. Song, C. Senanayake, J. Mulder, 2014, Organic letters.

Rhodium‐Catalyzed Asymmetric Allenylation of Sulfonylimines and Application to the Stereospecific Allylic Allenylation

Jinhua J. Song, C. Senanayake, N. Yee, 2016 .

Application of Newly Developed Anti-Selective Aldol Methodology: Synthesis of C6−C13 and C19−C28 Fragments of Miyakolide

Jinhua J. Song, Guoqiang Wang, S. Masamune, 1997 .

Direct conversion of primary and secondary carboxylic acids to trifluoromethyl ketones

Jinhua J. Song, C. Senanayake, F. Gallou, 2007 .

Acid-promoted SN1/E1 fragmentation/dimerization of 2-cumylmalonates

Jinhua J. Song, C. Senanayake, N. Yee, 2009 .

Room temperature palladium-catalyzed cross coupling of aryltrimethylammonium triflates with aryl Grignard reagents.

Jinhua J. Song, C. Senanayake, N. Yee, 2010, Organic letters.

N-heterocyclic carbene catalyzed trifluoromethylation of carbonyl compounds.

Jinhua J. Song, C. Senanayake, F. Gallou, 2005, Organic letters.

The first solid enols of anhydrides. Structure, properties, and enol/anhydride equilibria(1).

Jinhua J. Song, Z. Rappoport, Y. Lei, 2007, The Journal of organic chemistry.

Dialkoxyphosphinyl-substituted enols of carboxamides.

Jinhua J. Song, H. Yamataka, Z. Rappoport, 2007, The Journal of organic chemistry.

A general synthesis of substituted formylpyrroles from ketones and 4-formyloxazole.

Jinhua J. Song, C. Senanayake, N. Yee, 2007, Organic letters.

Development of a preparative-scale asymmetric synthesis of (R)-p-tolyl methyl sulfoxide for use in a one-pot synthesis of a drug intermediate containing a trifluoromethyl-substituted alcohol functionality

Jinhua J. Song, C. Senanayake, N. Yee, 2007 .

Scalable Process of Spiro(cyclopropane)oxazepane Pyridine Carboxylic Acid through Kulinkovich, Mitsunobu, and Pd-Catalyzed Intramolecular C–N Coupling

Jinhua J. Song, C. Senanayake, B. Qu, 2022, Organic Process Research & Development.

Asymmetric Synthesis of Active Pharmaceutical Ingredients

Jinhua J. Song, C. Senanayake, V. Farina, 2006 .

Development of an Efficient Synthesis of (2-Aminopyrimidin-5-yl) Boronic Acid

Jinhua J. Song, C. Senanayake, J. Mulder, 2016 .

A scalable and regioselective synthesis of 2-difluoromethyl pyridines from commodity chemicals.

Jinhua J. Song, C. Senanayake, Xudong Wei, 2014, Organic letters.

Discovery and optimization of p38 inhibitors via computer-assisted drug design.

Angela Berry, Jinhua J. Song, Ming-Hong Hao, 2007, Journal of medicinal chemistry.

Development and Characterization of a Cocrystal as a Viable Solid Form for an Active Pharmaceutical Ingredient

Jinhua J. Song, H. Nar, C. Senanayake, 2013 .

9.19 Synthesis of the Leading HCV Protease Inhibitors

Jinhua J. Song, C. Senanayake, N. Yee, 2012 .

Nickel-catalyzed C-3 direct arylation of pyridinium ions for the synthesis of 1-azafluorenes

Jinhua J. Song, C. Senanayake, M. Kozlowski, 2016, Chemical science.

Synthesis of 5-bromopyridyl-2-magnesium chloride and its application in the synthesis of functionalized pyridines.

Jinhua J. Song, C. Senanayake, Jinghua Xu, 2004, Organic Letters.

Synthesis of 5‐Bromopyridyl‐2‐magnesium Chloride and Its Application in the Synthesis of Functionalized Pyridines

Jinhua J. Song, C. Senanayake, Jinghua Xu, 2005 .

Process safety evaluation of a magnesium : Iodine exchange reaction

Jinhua J. Song, C. Senanayake, N. Yee, 2006 .

1,3‐Di‐tert‐butylimidazol‐2‐ylidene

Jinhua J. Song, C. Senanayake, N. Yee, 2008 .

Development of an Asymmetric Acetate Aldol Reaction with a Trifluoromethyl Ketone

Jinhua J. Song, C. Senanayake, Jinghua Xu, 2007 .

Modular Dihydrobenzoazaphosphole Ligands for Suzuki–Miyaura Cross-Coupling

Jinhua J. Song, C. Senanayake, N. Yee, 2018, Synthesis.

BABIPhos Family of Biaryl Dihydrobenzooxaphosphole Ligands for Asymmetric Hydrogenation.

Jinhua J. Song, C. Senanayake, N. Yee, 2018, Organic letters.

Heart-Cutting Two-Dimensional Ultrahigh-Pressure Liquid Chromatography for Process Development: Asymmetric Reaction Monitoring

Jinhua J. Song, C. Senanayake, Shaun Mendonsa, 2013 .

Atom-Economical Cross-Coupling of Internal and Terminal Alkynes to Access 1,3-Enynes.

Jinhua J. Song, C. Senanayake, K. Engle, 2020, Journal of the American Chemical Society.

Cu-Catalyzed Asymmetric Aminoboration of E-Vinylarenes with pivZPhos as the Ligand.

Jinhua J. Song, C. Senanayake, M. Kozlowski, 2019, Organic letters.

Feed-Forward Neural Network for Predicting Enantioselectivity of the Asymmetric Negishi Reaction

Jinhua J. Song, V. Batista, R. Crabtree, 2023, ACS central science.

Trifluoromethyl ketones from enolizable carboxylic acids via enediolate trifluoroacetylation/decarboxylation.

Jinhua J. Song, C. Senanayake, N. Yee, 2008, The Journal of organic chemistry.

Development of a Scalable Synthesis toward a KRAS G12C Inhibitor Building Block Bearing an All-Carbon Quaternary Stereocenter, Part 1: From Discovery Route to Kilogram-Scale Production

Jinhua J. Song, Denis Byrne, Joe Johnson, 2024, Organic Process Research & Development.

A practical and improved synthesis of (3S,5S)-3-[(tert-butyloxycarbonyl)methyl]- 5-[(methanesulfonyloxy)methyl]-2- pyrrolidinone.

Jinhua J. Song, N. Yee, S. Kapadia, 2002, The Journal of organic chemistry.

Development of a Scalable Synthesis toward a KRAS G12C Inhibitor Building Block Bearing an All-Carbon Quaternary Stereocenter, Part 2: Asymmetric Synthesis via Shi Epoxidation

Jinhua J. Song, F. Buono, Jon C. Lorenz, 2024, Organic Process Research & Development.