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A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow

Science (American Association for the Advancement of Science), 2018-01, Vol.359 (6374), p.429-434

2018

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Strain-release amination

Science (American Association for the Advancement of Science), 2016-01, Vol.351 (6270), p.241-246

2016

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Visible‐Light‐Initiated Manganese Catalysis for C−H Alkylation of Heteroarenes: Applications and Mechanistic Studies

Angewandte Chemie International Edition, 2017-11, Vol.56 (48), p.15309-15313

International ed. in English, 2017

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The Use of Copper Flow Reactor Technology for the Continuous Synthesis of 1,4‐Disubstituted 1,2,3‐Triazoles

Advanced synthesis & catalysis, 2009-04, Vol.351 (6), p.849-854

2009

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Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity

Journal of the American Chemical Society, 2017-03, Vol.139 (8), p.3209-3226

2017

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Organic chemistry. Strain-release amination

Science (American Association for the Advancement of Science), 2016-01, Vol.351 (6270), p.241-246

2016

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Electrochemically Driven, Ni-Catalyzed Aryl Amination: Scope, Mechanism, and Applications

Journal of the American Chemical Society, 2019-04, Vol.141 (15), p.6392-6402

2019

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High‐Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates

Angewandte Chemie International Edition, 2019-12, Vol.58 (51), p.18405-18409

International ed. in English, 2019

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Practical and innate carbon―hydrogen functionalization of heterocycles

Nature (London), 2012-12, Vol.492 (7427), p.95-99

2012

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Reductant‐Free Cross‐Electrophile Synthesis of Di(hetero)arylmethanes by Palladium‐Catalyzed Desulfinative C−C Coupling

Angewandte Chemie International Edition, 2022-05, Vol.61 (19), p.e202116775-n/a

International ed. in English, 2022

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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations

Journal of medicinal chemistry, 2014-06, Vol.57 (11), p.4720-4744

2014

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Rhodium(III)-Catalyzed C–H Activation: Ligand-Controlled Regioselective Synthesis of 4‑Methyl-Substituted Dihydroisoquinolones

Organic letters, 2019-07, Vol.21 (14), p.5689-5693

2019

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Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners

Angewandte Chemie (International ed.), 2016-03, Vol.55 (11), p.3590-3595

International ed. in English, 2016

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Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes

ACS catalysis, 2022-01, Vol.12 (1), p.600-606

2022

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Probing the chemical ‘reactome’ with high-throughput experimentation data

Nature chemistry, 2024-04, Vol.16 (4), p.633-643

2024

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Base‐Activated Latent Heteroaromatic Sulfinates as Nucleophilic Coupling Partners in Palladium‐Catalyzed Cross‐Coupling Reactions

Angewandte Chemie International Edition, 2021-10, Vol.60 (41), p.22461-22468

International ed. in English, 2021

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Copper-Catalyzed Synthesis of Masked (Hetero)Aryl Sulfinates

Organic letters, 2024-04, Vol.26 (14), p.2817-2820

2024

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Highly Modular Synthesis of 1,2-Diketones via Multicomponent Coupling Reactions of Isocyanides as CO Equivalents

ACS catalysis, 2019-05, Vol.9 (5), p.4508-4515

2019

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Identification of parallel medicinal chemistry protocols to expand branched amine design space

Organic & biomolecular chemistry, 2022-05, Vol.2 (18), p.3747-3754

2022

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Scalable Synthesis of 1-Bicyclo[1.1.1]pentylamine via a Hydrohydrazination Reaction

Organic letters, 2011-09, Vol.13 (17), p.4746-4748

2011

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Discovery of N‑((3R,4R)‑4-Fluoro-1-(6-((3-methoxy-1-methyl‑1H‑pyrazol-4-yl)amino)-9-methyl‑9H‑purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.3002-3019

2017

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A Parallel Approach to 7‑(Hetero)arylpyrazolo[1,5‑a]pyrimidin-5-ones

ACS combinatorial science, 2018-05, Vol.20 (5), p.256-260

2018

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Practical Kilogram Synthesis of (S)‑1-Benzyl-4-Bromo-3-Methyl-1,2,3,6-Tetrahydropyridine

Organic process research & development, 2021-10, Vol.25 (10), p.2315-2322

2021

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Synthesis of Pyridopyrazine-1,6-dione γ‑Secretase Modulators via Selective 4‑Methylimidazole N 1‑Buchwald Arylation

Journal of organic chemistry, 2019-04, Vol.84 (8), p.4921-4925

2019

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A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow

Strain-release amination

Visible‐Light‐Initiated Manganese Catalysis for C−H Alkylation of Heteroarenes: Applications and Mechanistic Studies

The Use of Copper Flow Reactor Technology for the Continuous Synthesis of 1,4‐Disubstituted 1,2,3‐Triazoles

Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity

Organic chemistry. Strain-release amination

Electrochemically Driven, Ni-Catalyzed Aryl Amination: Scope, Mechanism, and Applications

High‐Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates

Practical and innate carbon―hydrogen functionalization of heterocycles

Reductant‐Free Cross‐Electrophile Synthesis of Di(hetero)arylmethanes by Palladium‐Catalyzed Desulfinative C−C Coupling

Rhodium(III)-Catalyzed C–H Activation: Ligand-Controlled Regioselective Synthesis of 4‑Methyl-Substituted Dihydroisoquinolones

Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners

Automated Nanomole-Scale Reaction Screening toward Benzoate Bioisosteres: A Photocatalyzed Approach to Highly Elaborated Bicyclo[1.1.1]Pentanes

Probing the chemical ‘reactome’ with high-throughput experimentation data

Base‐Activated Latent Heteroaromatic Sulfinates as Nucleophilic Coupling Partners in Palladium‐Catalyzed Cross‐Coupling Reactions

Copper-Catalyzed Synthesis of Masked (Hetero)Aryl Sulfinates

Highly Modular Synthesis of 1,2-Diketones via Multicomponent Coupling Reactions of Isocyanides as CO Equivalents

Identification of parallel medicinal chemistry protocols to expand branched amine design space

Scalable Synthesis of 1-Bicyclo[1.1.1]pentylamine via a Hydrohydrazination Reaction

A Parallel Approach to 7‑(Hetero)arylpyrazolo[1,5‑a]pyrimidin-5-ones

Practical Kilogram Synthesis of (S)‑1-Benzyl-4-Bromo-3-Methyl-1,2,3,6-Tetrahydropyridine

Synthesis of Pyridopyrazine-1,6-dione γ‑Secretase Modulators via Selective 4‑Methylimidazole N 1‑Buchwald Arylation

Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib

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