The importance of synthetic chemistry in the pharmaceutical industry

Organic synthesis provides opportunities to transform drug discovery

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

Predicting reaction performance in C–N cross-coupling using machine learning

(2018) Derek T. Ahneman et al.   SCIENCE

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

(2018) Damith Perera et al.   SCIENCE

Mapping the dark space of chemical reactions with extended nanomole synthesis and MALDI-TOF MS

(2018) Shishi Lin et al.   SCIENCE

Nanoscale synthesis and affinity ranking

(2018) Nathan J. Gesmundo et al.   NATURE

Planning chemical syntheses with deep neural networks and symbolic AI

(2018) Marwin H. S. Segler et al.   NATURE

Unlocking P(V): Reagents for chiral phosphorothioate synthesis

(2018) Kyle W. Knouse et al.   SCIENCE

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

(2017) Tim Cernak et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Method for Identifying and Developing Functional Group Tolerant Catalytic Reactions: Application to the Buchwald–Hartwig Amination

(2017) Jeffery Richardson et al.   JOURNAL OF ORGANIC CHEMISTRY

Control of phosphorothioate stereochemistry substantially increases the efficacy of antisense oligonucleotides

(2017) Naoki Iwamoto et al.   NATURE BIOTECHNOLOGY

A multifunctional catalyst that stereoselectively assembles prodrugs

(2017) Daniel A. DiRocco et al.   SCIENCE

Biocatalysis in the Pharmaceutical Industry: The Need for Speed

(2017) Matthew D. Truppo   ACS Medicinal Chemistry Letters

Prediction of Organic Reaction Outcomes Using Machine Learning

(2017) Connor W. Coley et al.   ACS Central Science

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

(2016) Paula Ruiz-Castillo 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

Strain-release amination

(2016) R. Gianatassio et al.   SCIENCE

Aryl amination using ligand-free Ni(II) salts and photoredox catalysis

(2016) Emily B. Corcoran et al.   SCIENCE

Chemistry informer libraries: a chemoinformatics enabled approach to evaluate and advance synthetic methods

(2016) Peter S. Kutchukian et al.   Chemical Science

Reinventing Chemistry

(2015) George M. Whitesides   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?

(2015) Dean G. Brown et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemistry: Why synthesize?

(2015) Philip Ball   NATURE

Switching on elusive organometallic mechanisms with photoredox catalysis

(2015) Jack A. Terrett et al.   NATURE

Development of a Direct Photocatalytic C–H Fluorination for the Preparative Synthesis of Odanacatib

(2015) Shira D. Halperin et al.   ORGANIC LETTERS

Recent advances in engineering proteins for biocatalysis

(2014) Ye Li et al.   BIOTECHNOLOGY AND BIOENGINEERING

Discovery and Development of Simeprevir (TMC435), a HCV NS3/4A Protease Inhibitor

(2014) Åsa Rosenquist et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

(2014) Edon Vitaku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Contemporary screening approaches to reaction discovery and development

(2014) Karl D. Collins et al.   Nature Chemistry

Late-Stage Fluorination: From Fundamentals to Application

(2014) Michael G. Campbell et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Nanomole-scale high-throughput chemistry for the synthesis of complex molecules

(2014) A. Buitrago Santanilla et al.   SCIENCE

Location Matters: Site of Conjugation Modulates Stability and Pharmacokinetics of Antibody Drug Conjugates

(2013) Pavel Strop et al.   CHEMISTRY & BIOLOGY

A robustness screen for the rapid assessment of chemical reactions

(2013) Karl D. Collins et al.   Nature Chemistry

Ribosomal production and in vitro selection of natural product-like peptidomimetics: The FIT and RaPID systems

(2012) Christopher J Hipolito et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

The enumeration of chemical space

(2012) Jean-Louis Reymond et al.   Wiley Interdisciplinary Reviews-Computational Molecular Science

Discovery of Vaniprevir (MK-7009), a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor

(2010) John A. McCauley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biocatalytic Asymmetric Synthesis of Chiral Amines from Ketones Applied to Sitagliptin Manufacture

(2010) C. K. Savile et al.   SCIENCE

Bioorthogonal Chemistry: Fishing for Selectivity in a Sea of Functionality

(2009) Ellen M. Sletten et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Phage-encoded combinatorial chemical libraries based on bicyclic peptides

(2009) Christian Heinis et al.   Nature Chemical Biology

Solid-Phase Synthesis of Stereoregular Oligodeoxyribonucleoside Phosphorothioates Using Bicyclic Oxazaphospholidine Derivatives as Monomer Units

(2008) Natsuhisa Oka et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY