Kilogram-Scale Preparation of an Aminopyrazole Building Block via Copper-Catalyzed Aryl Amidation

Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

(2020) Chaomin Li et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Recent Advances in Synthesis and Properties of Nitrated-Pyrazoles Based Energetic Compounds

(2020) Shijie Zhang et al.   MOLECULES

Early Process Development of an Irreversible Epidermal Growth Factor Receptor (EGFR) T790 M Inhibitor

(2019) Yong Tao et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Selective Reduction of Nitroarenes Catalyzed by Sustainable and Reusable DNA-supported Nickel Nanoparticles in Water at Room Temperature

(2019) Mahsa Niakan et al.   CATALYSIS LETTERS

Streamlined Synthesis of Diaminopyridines via Pd‐Catalyzed Ammonia Coupling with Deactivated Amino‐Chloropyridines

(2019) Serena Fantasia et al.   CHEMISTRY-A EUROPEAN JOURNAL

Cu-Catalyzed Couplings of Heteroaryl Primary Amines and (Hetero)aryl Bromides with 6-Hydroxypicolinamide Ligands

(2019) David J. Bernhardson et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Nickel-Catalyzed C–N Cross-Coupling of Ammonia, (Hetero)anilines, and Indoles with Activated (Hetero)aryl Chlorides Enabled by Ligand Design

(2019) Ryan T. McGuire et al.   ACS Catalysis

A toxicogenomic approach for the risk assessment of the food contaminant acetamide

(2019) Rance Nault et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Discovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor

(2018) Jaebong Jang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Potential impurities in drug substances: Compound-specific toxicology limits for 20 synthetic reagents and by-products, and a class-specific toxicology limit for alkyl bromides

(2018) J.P. Bercu et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

(2018) Andrew Fensome et al.   JOURNAL OF MEDICINAL CHEMISTRY

N,N′-Bisoxalamides Enhance the Catalytic Activity in Cu-Catalyzed Coupling of (Hetero)Aryl Bromides with Anilines and Secondary Amines

(2017) Subhajit Bhunia et al.   JOURNAL OF ORGANIC CHEMISTRY

Catalytic Reductions and Tandem Reactions of Nitro Compounds Using in Situ Prepared Nickel Boride Catalyst in Nanocellulose Solution

(2017) Kaniraj Jeya Prathap et al.   ORGANIC LETTERS

Discovery of N-(Naphthalen-1-yl)-N′-alkyl Oxalamide Ligands Enables Cu-Catalyzed Aryl Amination with High Turnovers

(2017) Jie Gao et al.   ORGANIC LETTERS

Copper-Catalyzed Coupling Reaction of (Hetero)Aryl Chlorides and Amides

(2017) Subhadip De et al.   ORGANIC LETTERS

Origins of high catalyst loading in copper(i)-catalysed Ullmann–Goldberg C–N coupling reactions

(2017) Grant J. Sherborne et al.   Chemical Science

Ni-Catalyzed Amination Reactions: An Overview

(2016) Mario Marín et al.   CHEMICAL RECORD

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

(2016) Paula Ruiz-Castillo et al.   CHEMICAL REVIEWS

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

(2016) Hengmiao Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Developments in the Reduction of Aromatic and Aliphatic Nitro Compounds to Amines

(2016) Manuel Orlandi et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Nickel-Catalyzed Amination of Aryl Chlorides with Ammonia or Ammonium Salts

(2015) Rebecca A. Green et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Genotoxic Impurities in Pharmaceutical Manufacturing: Sources, Regulations, and Mitigation

(2015) Gyorgy Szekely et al.   CHEMICAL REVIEWS

Assembly of Primary (Hetero)Arylamines via CuI/Oxalic Diamide-Catalyzed Coupling of Aryl Chlorides and Ammonia

(2015) Mengyang Fan et al.   ORGANIC LETTERS

Selective reduction of nitro-compounds to primary amines by nickel-catalyzed hydrosilylative reduction

(2015) Shuai Sun et al.   RSC Advances

Copper catalysed Ullmann type chemistry: from mechanistic aspects to modern development

(2014) Carlo Sambiagio et al.   CHEMICAL SOCIETY REVIEWS

Iron-catalysed, general and operationally simple formal hydrogenation using Fe(OTf)3 and NaBH4

(2014) Alistair J. MacNair et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

C–N bond forming cross-coupling reactions: an overview

(2013) Jitender Bariwal et al.   CHEMICAL SOCIETY REVIEWS

Risk Assessment of Genotoxic Impurities in New Chemical Entities: Strategies To Demonstrate Control

(2013) Andrew Teasdale et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

The Complementary Competitors: Palladium and Copper in C–N Cross-Coupling Reactions

(2012) Irina P. Beletskaya et al.   ORGANOMETALLICS

Palladium- and copper-mediatedN-aryl bond formation reactions for the synthesis of biological active compounds

(2011) Carolin Fischer et al.   Beilstein Journal of Organic Chemistry

Efficient synthesis of biazoles by aerobic oxidative homocoupling of azoles catalyzed by a copper(i)/2-pyridonate catalytic system

(2011) Mingwen Zhu et al.   CHEMICAL COMMUNICATIONS

General and Selective Iron-Catalyzed Transfer Hydrogenation of Nitroarenes without Base

(2011) Gerrit Wienhöfer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Catalytic Organometallic Reactions of Ammonia

(2010) Jessica L. Klinkenberg et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Copper-MediatedN-Heteroarylation of Primary Sulfonamides: Synthesis of Mono-N-heteroaryl Sulfonamides

(2010) Jonathan Baffoe et al.   ORGANIC LETTERS

Process Development and Large-Scale Synthesis of a c-Met Kinase Inhibitor

(2010) Gavin W. Stewart et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Monitoring and Control of Genotoxic Impurity Acetamide in the Synthesis of Zaurategrast Sulfate

(2010) Arnaud Schülé et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Risk Assessment of Potentially Genotoxic Impurities within the Framework of Quality by Design

(2010) Adam R. Looker et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Genotoxic Impurities: From Structural Alerts to Qualification

(2010) David J. Snodin   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Diamine ligands in copper-catalyzed reactions

(2010) David S. Surry et al.   Chemical Science

Dialkylbiaryl phosphines in Pd-catalyzed amination: a user's guide

(2010) David S. Surry et al.   Chemical Science

Recent Applications of Palladium-Catalyzed Coupling Reactions in the Pharmaceutical, Agrochemical, and Fine Chemical Industries

(2009) Christian Torborg et al.   ADVANCED SYNTHESIS & CATALYSIS

Easy Copper-Catalyzed Synthesis of Primary Aromatic Amines by Couplings Aromatic Boronic Acids with Aqueous Ammonia at Room Temperature

(2009) Honghua Rao et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic CC, CN, and CO Ullmann-Type Coupling Reactions

(2009) Florian Monnier et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Efficient copper-catalyzed coupling of aryl chlorides, bromides and iodides with aqueous ammonia

(2009) Hanhui Xu et al.   CHEMICAL COMMUNICATIONS

An Aromatic Glaser−Hay Reaction

(2009) Hien-Quang Do et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Palladium-Catalyzed Coupling of Ammonia with Aryl Chlorides, Bromides, Iodides, and Sulfonates: A General Method for the Preparation of Primary Arylamines

(2009) Giang D. Vo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An efficient and convenient Cu(OAc)2/air mediated oxidative coupling of azoles via C–H activation

(2009) Yan Li et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Oxidative dimerization of azoles via copper(II)/silver(I)-catalyzed CH homocoupling

(2009) Daiki Monguchi et al.   TETRAHEDRON LETTERS

Copper/Amino Acid Catalyzed Cross-Couplings of Aryl and Vinyl Halides with Nucleophiles†

(2008) Dawei Ma et al.   ACCOUNTS OF CHEMICAL RESEARCH

A Very Simple Copper-Catalyzed Synthesis of Anilines by Employing Aqueous Ammonia

(2008) Ning Xia et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Copper-Mediated Coupling Reactions and Their Applications in Natural Products and Designed Biomolecules Synthesis

(2008) Gwilherm Evano et al.   CHEMICAL REVIEWS

Copper Complexes of Anionic Nitrogen Ligands in the Amidation and Imidation of Aryl Halides

(2008) Jesse W. Tye et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mechanistic Studies on the Copper-CatalyzedN-Arylation of Amides

(2008) Eric R. Strieter et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY