J. Alcázar

发表

Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging.

G. Bormans, X. Langlois, H. Lavreysen, 2012, Journal of medicinal chemistry.

What We Observe In Vivo Is Not Always What We See In Vitro: Development and Validation of 11C-JNJ-42491293, A Novel Radioligand for mGluR2

Mark E. Schmidt, G. Bormans, X. Langlois, 2017, The Journal of Nuclear Medicine.

Visible-Light-Induced Nickel-Catalyzed Negishi Cross-Couplings by Exogenous-Photosensitizer-Free Photocatalysis.

A. Fontana, A. de la Hoz, J. Alcázar, 2018, Angewandte Chemie.

Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles

Á. Díaz‐Ortiz, J. Alcázar, M. Berton, 2017 .

Improving the throughput of batch photochemical reactions using flow: Dual photoredox and nickel catalysis in flow for C(sp2)C(sp3) cross-coupling.

J. Alcázar, Irini Abdiaj, 2016, Bioorganic & medicinal chemistry.

Sustainable Flow Chemistry in Drug Discovery

J. Alcázar, 2017 .

Scalability of Visible-Light-Induced Nickel Negishi Reactions: A Combination of Flow Photochemistry, Use of Solid Reagents, and In-Line NMR Monitoring.

J. Alcázar, Irini Abdiaj, C. Horn, 2018, The Journal of organic chemistry.

Synergy between supported ionic liquid-like phases and immobilized palladium N-heterocyclic carbene–phosphine complexes for the Negishi reaction under flow conditions

E. García‐Verdugo, S. Luis, Raúl Porcar, 2020, Beilstein journal of organic chemistry.

Microwave‐Assisted Continuous Flow Organic Synthesis (MACOS)

J. Alcázar, J. M. Muñoz, 2013 .

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.

J. Bartolomé-Nebreda, Sergio A Alonso de Diego, M. Martín-Martín, 2016, Bioorganic & medicinal chemistry letters.

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.

A. Megens, X. Langlois, J. Bartolomé-Nebreda, 2015, ACS medicinal chemistry letters.

Negishi coupling reactions with [11C]CH3I: a versatile method for efficient 11C-C bond formation.

J. Llop, A. Arrieta, F. Cossío, 2018, Chemical communications.

Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.

P. Bonaventure, N. Carruthers, Hong Ao, 2015, Bioorganic & medicinal chemistry letters.

Visible-Light-Induced Trifluoromethylation of Highly Functionalized Arenes and Heteroarenes in Continuous Flow

J. Alcázar, Irini Abdiaj, C. Bottecchia, 2017, Synthesis.

Photoinduced Palladium-Catalyzed Negishi Cross-Couplings Enabled by the Visible-Light Absorption of Palladium-Zinc Complexes.

A. de la Hoz, Á. Díaz‐Ortiz, J. Alcázar, 2018, Angewandte Chemie.

Photoinduced Palladium‐Catalyzed Negishi Cross‐Couplings Enabled by the Visible‐Light Absorption of Palladium–Zinc Complexes

Á. Díaz‐Ortiz, J. Alcázar, M. V. Gomez, 2018, Angewandte Chemie.

Preclinical Evaluation of a P2X7 Receptor–Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates

W. Vanduffel, G. Bormans, X. Langlois, 2016, The Journal of Nuclear Medicine.

Continuous Synthesis of Organozinc Halides Coupled to Negishi Reactions

D. T. McQuade, J. Alcázar, Nerea Alonso, 2014 .

Recent advances in positron emission tomography (PET) radiotracers for imaging phosphodiesterases.

G. Bormans, S. Celen, J. Andrés, 2012, Current topics in medicinal chemistry.

First Example of a Continuous-Flow Carbonylation Reaction Using Aryl Formates as CO Precursors

Á. Díaz‐Ortiz, J. Alcázar, Nerea Alonso, 2014, Journal of Flow Chemistry.

Application of Flow Chemistry to the Selective Reduction of Esters to Aldehydes

Á. Díaz‐Ortiz, J. Alcázar, J. M. Muñoz, 2012 .

Application of flow chemistry to the reduction of nitriles to aldehydes

Á. Díaz‐Ortiz, J. Alcázar, J. M. Muñoz, 2011 .

Grignard Reagents on a Tab: Direct Magnesium Insertion under Flow Conditions.

A. de la Hoz, Á. Díaz‐Ortiz, J. Alcázar, 2017, Organic letters.

Cross‐Coupling in Flow using Supported Catalysts: Mild, Clean, Efficient and Sustainable Suzuki–Miyaura Coupling in a Single Pass

Á. Díaz‐Ortiz, J. Alcázar, J. M. Muñoz, 2012 .

Synthesis of imidazole N-oxides in solvent-free conditions

J. Alcázar, M. Begtrup, A. Hoz, 1996 .

C( sp 3 )−C( sp 3 ) Bond Formation via Electrochemical Alkoxylation and Subsequent Lewis Acid Promoted Reactions

Á. Díaz‐Ortiz, J. Alcázar, Alessia Petti, 2021, Advanced Synthesis & Catalysis.

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.

M. Bakker, A. Megens, J. M. Alonso, 2005, Journal of medicinal chemistry.

Flow Chemistry in Drug Discovery: Challenges and Opportunities

Enol López, Jesús Alcázar, J. Alcázar, 2021 .

Chapter Four - Recent Advances of Microfluidics Technologies in the Field of Medicinal Chemistry

Jesus Alcazar, György Dormán, Laszlo Urge, 2017 .

Recent applications of microwave irradiation to medicinal chemistry.

J. Alcázar, Daniel Oehlrich, 2010, Future medicinal chemistry.

Reproducibility and Scalability of Microwave-Assisted Reactions

José M. Carrillo, Antonio de la Hoz, Angel Díaz-Ortiz, 2011 .

Reproducibility across Microwave Instruments: First Example of Genuine Parallel Scale up of Compounds under Microwave Irradiation

J. Alcázar, G. Diels, B. Schoentjes, 2004 .

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.

M. Bakker, A. Megens, R. Álvarez, 2004, Bioorganic & medicinal chemistry letters.

On-demand synthesis of organozinc halides under continuous flow conditions

J. Alcázar, M. Berton, L. Huck, 2018, Nature Protocols.

Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.

Julen Oyarzabal, Trevor Howe, I. van der Linden, 2009, Journal of medicinal chemistry.

Practical preparation of challenging amides from non-nucleophilic amines and esters under flow conditions.

F. Delgado, J. Alcázar, W. D. De Borggraeve, 2014, Chemical communications.

Preparation of amides mediated by isopropylmagnesium chloride under continuous flow conditions

Jesús Alcázar, Antonio de la Hoz, Angel Díaz-Ortiz, 2012 .

Visible‐Light‐Promoted Iron‐Catalyzed C(sp2)–C(sp3) Kumada Cross‐Coupling in Flow

E. Zysman‐Colman, J. Alcázar, T. Noël, 2019, Angewandte Chemie (International Ed. in English).

A biomimetic SH2 cross-coupling mechanism for quaternary sp3-carbon formation

J. Alcázar, Wei Liu, D. MacMillan, 2021, Science.

Formation of quaternary carbons through cobalt-catalyzed C(sp3)-C(sp3) Negishi cross-coupling.

A. de la Hoz, Á. Díaz‐Ortiz, J. Alcázar, 2020, Chemical communications.

End-to-End Automated Synthesis of C(sp3)-Enriched Drug-like Molecules via Negishi Coupling and Novel, Automated Liquid-Liquid Extraction.

María Lourdes Linares, A. Fontana, J. Alcázar, 2022, Journal of medicinal chemistry.

First Example of Alkyl–Aryl Negishi Cross-Coupling in Flow: Mild, Efficient and Clean Introduction of Functionalized Alkyl Groups

Á. Díaz‐Ortiz, J. Alcázar, Nerea Alonso, 2015, Journal of Flow Chemistry.

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

Kari A. Johnson, K. Gregory, J. Bartolomé-Nebreda, 2015, Neuron.

Synthesis of imidazole 1-oxides from 1,2-diimines

J. Alcázar, M. Begtrup, A. Hoz, 1995 .

Synthesis of novel aza analogues of 2-substituted-2,3-dihydro-1,4-benzodioxins as potential new scaffolds for drug discovery

J. Andrés, J. Alcázar, K. V. Emelen, 2003 .

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.

J. Bartolomé-Nebreda, Carlos M Martínez-Viturro, G. Macdonald, 2015, Bioorganic & medicinal chemistry letters.

Synthesis of novel 3-substituted-2,3-dihydro-1,4-dioxino[2,3-b]pyridines as potential new scaffolds for drug discovery: selective introduction of substituents on the pyridine ring

J. M. Alonso, J. Alcázar, L. Iturrino, 2003 .

Synthesis of Novel 3‐Substituted‐2,3‐dihydro‐1,4‐dioxino[2,3‐b]pyridines as Potential New Scaffolds for Drug Discovery: Selective Introduction of Substituents on the Pyridine Ring.

J. M. Alonso, J. Alcázar, L. Iturrino, 2004 .

Novel analogues of 3-substituted-2,3-dihydro-1,4-dioxino[2,3-b]pyridines: modifications in the dioxane ring

J. Andrés, J. Alcázar, K. V. Emelen, 2003 .

Novel Analogues of 3-Substituted-2,3-dihydro-1,4-dioxino[2,3-b]pyridines: Modifications in the Dioxane Ring.

J. Andrés, J. Alcázar, K. V. Emelen, 2004 .

Blocking melanin-concentrating hormone MCH1 receptor affects rat sleep-wake architecture.

T. Steckler, W. Drinkenburg, J. Alcázar, 2008, European journal of pharmacology.

Comparison of New Tau PET-Tracer Candidates With [18F]T808 and [18F]T807

R. Vandenberghe, G. Bormans, K. Van Laere, 2016, Molecular imaging.

Preclinical evaluation of [18F]JNJ42259152 as a PET tracer for PDE10A

Mark Schmidt, Koen Van Laere, Guy Bormans, 2013, NeuroImage.

Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.

G. Bormans, X. Langlois, G. Vanhoof, 2011, Journal of medicinal chemistry.

Preclinical Evaluation of 18F-JNJ41510417 as a Radioligand for PET Imaging of Phosphodiesterase-10A in the Brain

Koen Van Laere, Guy Bormans, Sofie Celen, 2010, The Journal of Nuclear Medicine.

Cover Picture: Continuous Synthesis of Organozinc Halides Coupled to Negishi Reactions (Adv. Synth. Catal. 18/2014)

D. T. McQuade, J. Alcázar, Nerea Alonso, 2014 .

Visible‐Light‐Promoted Iron‐Catalyzed C(sp 2 )–C(sp 3 ) Kumada Cross‐Coupling in Flow

E. Zysman‐Colman, J. Alcázar, T. Noël, 2019, Angewandte Chemie.

Challenge and opportunity: The two edges of continuous-flow photochemistry

J. Alcázar, Gabriela Oksdath-Mansilla, F. Bisogno, 2023, Chem Catalysis.

Visible Light-Induced Nickel-Catalyzed Negishi Cross-Coupling . A New Approach to Exogenous Photosensitizer-free Photocatalysis

A. Fontana, J. Alcázar, Irini Abdiaj, 2018 .

Synthesis of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives displaying combined alpha2-adrenoceptor antagonistic and 5-HT reuptake inhibiting activities.

A. Megens, J. M. Alonso, J. Andrés, 2006, Bioorganic & medicinal chemistry.

Flow chemistry as a tool to access novel chemical space for drug discovery.

Enol López, María Lourdes Linares, Jesús Alcázar, 2020, Future medicinal chemistry.

Synthesis and structure–Activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT2A/2C receptor antagonists. Part 2

A. Megens, T. Meert, J. M. Alonso, 2002 .

Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.

María Lourdes Linares, J. M. Alonso, G. Macdonald, 2014, Journal of medicinal chemistry.

Fully Automated Flow Protocol for C(sp3)-C(sp3) Bond Formation from Tertiary Amides and Alkyl Halides.

María Lourdes Linares, A. de la Hoz, Á. Díaz‐Ortiz, 2023, Organic letters.

Synthesis of 4-hydroxylamino-1-azabuta-1,3-dienes and their cyclization to 2-substituted pyrazole 1-oxides

J. Alcázar, M. Begtrup, A. Hoz, 1995 .

Continuous-flow photochemistry as an automated platform integrated with closed-loop AI/ML approaches

J. Alcázar, Gabriela Oksdath-Mansilla, F. Bisogno, 2023, Chem Catalysis.

Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.

M. Bakker, A. Megens, X. Langlois, 2007, Bioorganic & medicinal chemistry.

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.

M. Bakker, A. Megens, J. M. Alonso, 2003, Bioorganic & medicinal chemistry letters.

Influence of polarity on the scalability and reproducibility of solvent-free microwave-assisted reactions.

A. Fontana, M. Herrero, A. de la Hoz, 2011, Combinatorial chemistry & high throughput screening.

Reproducibility and scalability of solvent-free microwave-assisted reactions: from domestic ovens to controllable parallel applications.

A. Fontana, A. de la Hoz, Á. Díaz‐Ortiz, 2007, Combinatorial chemistry & high throughput screening.

Reproducibility across microwave instruments: preparation of a set of 24 compounds on a multiwell plate under temperature-controlled conditions.

J. Alcázar, 2005, Journal of combinatorial chemistry.

De novo Design of Organic Photocatalysts: Bithiophene Derivatives for the Visible-light Induced C−H Functionalization of Heteroarenes

M. Blesa, J. Orduna, J. Alcázar, 2019, Advanced Synthesis & Catalysis.

J. Bartolomé-Nebreda, M. Martín-Martín, Carlos M Martínez-Viturro, 2016, Bioorganic & medicinal chemistry letters.

Discovery of a Series of Substituted 1H-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.

C. Dvorak, N. Carruthers, J. Alcázar, 2023, Journal of medicinal chemistry.

Visible-Light-Induced Nickel-Catalyzed Negishi Cross-Couplings by Exogenous-Photosensitizer-Free Photocatalysis.

A. Fontana, J. Alcázar, Irini Abdiaj, 2018, Angewandte Chemie.

Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.

G. Bormans, X. Langlois, G. Vanhoof, 2011, Journal of medicinal chemistry.

Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging.

G. Bormans, X. Langlois, H. Lavreysen, 2012, Journal of medicinal chemistry.