An overview of late-stage functionalization in today’s drug discovery

The importance of synthetic chemistry in the pharmaceutical industry

(2019) Kevin R. Campos et al.   SCIENCE

Pharmaceutical diversification via palladium oxidative addition complexes

(2019) Mycah R. Uehling et al.   SCIENCE

Late-Stage Functionalization of Drug-Like Molecules Using Diversinates

(2018) Christian A. Kuttruff et al.   ChemMedChem

Decarboxylative Trifluoromethylation of Aliphatic Carboxylic Acids

(2018) Jacob A. Kautzky et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Generating carbyne equivalents with photoredox catalysis

(2018) Zhaofeng Wang et al.   NATURE

Manganese-catalysed benzylic C(sp3)–H amination for late-stage functionalization

(2018) Joseph R. Clark et al.   Nature Chemistry

Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals

(2018) Marco Simonetti et al.   Nature Chemistry

Organic synthesis provides opportunities to transform drug discovery

(2018) David C. Blakemore et al.   Nature Chemistry

Direct heterobenzylic fluorination, difluorination and trifluoromethylthiolation with dibenzenesulfonamide derivatives

(2018) Michael Meanwell et al.   Chemical Science

Drug metabolism in drug discovery and development

(2018) Zhoupeng Zhang et al.   Acta Pharmaceutica Sinica B

Decarboxylative sp3 C–N coupling via dual copper and photoredox catalysis

(2018) Yufan Liang et al.   NATURE

Palladium-catalysed electrophilic aromatic C–H fluorination

(2018) Kumiko Yamamoto et al.   NATURE

Expanding the medicinal chemistry synthetic toolbox

(2018) Jonas Boström et al.   NATURE REVIEWS DRUG DISCOVERY

Exploration of new reaction tools for late-stage functionalization of complex chemicals

(2018) Alejandra Dominguez-Huerta et al.   CANADIAN JOURNAL OF CHEMISTRY

Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group

(2018) Jichen Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Alkyl Sulfinates: Radical Precursors Enabling Drug Discovery

(2018) Joel M. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Late-Stage Aromatic C–H Oxygenation

(2018) Jonas Börgel et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chemoselective methylene oxidation in aromatic molecules

(2018) Jinpeng Zhao et al.   Nature Chemistry

Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view

(2017) Navriti Chadha et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Enabling Efficient Late-Stage Functionalization of Drug-Like Molecules with LC-MS and Reaction-Driven Data Processing

(2017) Huifang Yao et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Remote, Late-Stage Oxidation of Aliphatic C–H Bonds in Amide-Containing Molecules

(2017) Takeshi Nanjo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Site-selective and stereoselective functionalization of non-activated tertiary C–H bonds

(2017) Kuangbiao Liao et al.   NATURE

Ligand-accelerated non-directed C–H functionalization of arenes

(2017) Peng Wang et al.   NATURE

Selective sp3 C–H alkylation via polarity-match-based cross-coupling

(2017) Chip Le et al.   NATURE

Direct α-C–H bond functionalization of unprotected cyclic amines

(2017) Weijie Chen et al.   Nature Chemistry

Metal-free C–H alkylation of heteroarenes with alkyltrifluoroborates: a general protocol for 1°, 2° and 3° alkylation

(2017) Jennifer K. Matsui et al.   Chemical Science

Accessing Drug Metabolites via Transition-Metal Catalyzed C−H Oxidation: The Liver as Synthetic Inspiration

(2016) Julien Genovino et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Modern Transition-Metal-Catalyzed Carbon–Halogen Bond Formation

(2016) David A. Petrone et al.   CHEMICAL REVIEWS

The medicinal chemist's toolbox for late stage functionalization of drug-like molecules

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

Photoredox-Catalyzed Hydroxymethylation of Heteroaromatic Bases

(2016) Chelsea A. Huff et al.   JOURNAL OF ORGANIC CHEMISTRY

Photoredox Catalysis in Organic Chemistry

(2016) Megan H. Shaw et al.   JOURNAL OF ORGANIC CHEMISTRY

C–H Xanthylation: A Synthetic Platform for Alkane Functionalization

(2016) William L. Czaplyski et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Site-selective and stereoselective functionalization of unactivated C–H bonds

(2016) Kuangbiao Liao et al.   NATURE

C–H functionalization of amines with aryl halides by nickel-photoredox catalysis

(2016) Derek T. Ahneman et al.   Chemical Science

Iridium-Catalyzed Silylation of Aryl C–H Bonds

(2015) Chen Cheng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Manganese-Catalyzed Late-Stage Aliphatic C–H Azidation

(2015) Xiongyi Huang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Evolution of C–H Bond Functionalization from Methane to Methodology

(2015) John F. Hartwig   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Alcohols as alkylating agents in heteroarene C–H functionalization

(2015) Jian Jin et al.   NATURE

Site-selective arene C-H amination via photoredox catalysis

(2015) N. A. Romero et al.   SCIENCE

Site-Selective Aliphatic C–H Bromination Using N-Bromoamides and Visible Light

(2014) Valerie A. Schmidt et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Catalyst-Controlled Aliphatic C–H Oxidations with a Predictive Model for Site-Selectivity

(2013) Paul E. Gormisky et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Palladium-Catalyzed Cross-Coupling: A Historical Contextual Perspective to the 2010 Nobel Prize

(2012) Carin C. C. Johansson Seechurn et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Oxidative Aliphatic C-H Fluorination with Fluoride Ion Catalyzed by a Manganese Porphyrin

(2012) W. Liu et al.   SCIENCE

Weak Coordination as a Powerful Means for Developing Broadly Useful C–H Functionalization Reactions

(2011) Keary M. Engle et al.   ACCOUNTS OF CHEMICAL RESEARCH

If CH Bonds Could Talk: Selective CH Bond Oxidation

(2011) Timothy Newhouse et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic Dehydrogenative Cross-Coupling: Forming Carbon−Carbon Bonds by Oxidizing Two Carbon−Hydrogen Bonds

(2011) Charles S. Yeung et al.   CHEMICAL REVIEWS

Halogen Atoms in the Modern Medicinal Chemistry: Hints for the Drug Design

(2010) Marcelo Hernandes et al.   CURRENT DRUG TARGETS

A Graphical Journey of Innovative Organic Architectures That Have Improved Our Lives

(2010) Nicholas A. McGrath et al.   JOURNAL OF CHEMICAL EDUCATION

Manganese Porphyrins Catalyze Selective C−H Bond Halogenations

(2010) Wei Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

How to improve R&D productivity: the pharmaceutical industry's grand challenge

(2010) Steven M. Paul et al.   NATURE REVIEWS DRUG DISCOVERY

Combined Effects on Selectivity in Fe-Catalyzed Methylene Oxidation

(2010) M. S. Chen et al.   SCIENCE

Strain Release in CH Bond Activation?

(2009) Ke Chen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Spending on new drug development

(2009) Christopher Paul Adams et al.   HEALTH ECONOMICS

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Many Roles for Fluorine in Medicinal Chemistry

(2008) William K. Hagmann   JOURNAL OF MEDICINAL CHEMISTRY