Cobalt-catalysed C–H methylation for late-stage drug diversification

Pharmaceutical diversification via palladium oxidative addition complexes

(2019) Mycah R. Uehling et al.   SCIENCE

Site-selective and versatile aromatic C−H functionalization by thianthrenation

(2019) Florian Berger et al.   NATURE

Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis

(2019) Stefan Bäurle et al.   JOURNAL OF MEDICINAL CHEMISTRY

High Throughput Reaction Screening with Nanomoles of Solid Reagents Coated on Glass Beads

(2019) Ying Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Selective formation of γ-lactams via C–H amidation enabled by tailored iridium catalysts

(2018) Seung Youn Hong et al.   SCIENCE

Enantioselective C(sp3)‒H bond activation by chiral transition metal catalysts

(2018) Tyler G. Saint-Denis et al.   SCIENCE

A comprehensive overview of directing groups applied in metal-catalysed C–H functionalisation chemistry

(2018) Carlo Sambiagio et al.   CHEMICAL SOCIETY REVIEWS

Nanoscale synthesis and affinity ranking

(2018) Nathan J. Gesmundo et al.   NATURE

Design of catalysts for site-selective and enantioselective functionalization of non-activated primary C–H bonds

(2018) Kuangbiao Liao et al.   Nature Chemistry

Inside Cover: Ultra-Tuning of the Aperture Size in Stiffened ZIF-8_Cm Frameworks with Mixed-Linker Strategy for Enhanced CO2 /CH4 Separation (Angew. Chem. Int. Ed. 1/2019)

(2018) Qianqian Hou et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

3d Transition Metals for C–H Activation

(2018) Parthasarathy Gandeepan et al.   CHEMICAL REVIEWS

Alkyl Sulfinates: Radical Precursors Enabling Drug Discovery

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

Trimethylphosphate as a Methylating Agent for Cross Coupling: A Slow-Release Mechanism for the Methylation of Arylboronic Esters

(2018) Zhi-Tao He et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2017) Chip Le et al.   NATURE

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

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

Iron-Catalyzed Ortho C–H Methylation of Aromatics Bearing a Simple Carbonyl Group with Methylaluminum and Tridentate Phosphine Ligand

(2016) Rui Shang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Palladium-catalysed transannular C–H functionalization of alicyclic amines

(2016) Joseph J. Topczewski et al.   NATURE

A general catalytic β-C–H carbonylation of aliphatic amines to β-lactams

(2016) Darren Willcox et al.   SCIENCE

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

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

Bidentate, Monoanionic Auxiliary-Directed Functionalization of Carbon–Hydrogen Bonds

(2015) Olafs Daugulis et al.   ACCOUNTS OF CHEMICAL RESEARCH

Iron-Catalyzed C(sp2)H and C(sp3)H Methylations of Amides and Anilides

(2015) Karolina Graczyk et al.   CHEMISTRY-A EUROPEAN JOURNAL

Cobalt-Catalyzed C–H Activation

(2015) Marc Moselage et al.   ACS Catalysis

Transition metal-catalyzed C–H bond functionalizations by the use of diverse directing groups

(2015) Zhengkai Chen et al.   Organic Chemistry Frontiers

Iridium-Catalyzed C–H Borylation of Heteroarenes: Scope, Regioselectivity, Application to Late-Stage Functionalization, and Mechanism

(2014) Matthew A. Larsen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design of Experiments (DoE) and Process Optimization. A Review of Recent Publications

(2014) Steven A. Weissman et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

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

(2014) A. Buitrago Santanilla et al.   SCIENCE

CH Functionalization Logic Enables Synthesis of (+)-Hongoquercin A and Related Compounds

(2013) Brandon R. Rosen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Profound Methyl Effects in Drug Discovery and a Call for New CH Methylation Reactions

(2013) Heike Schönherr et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic Functionalization of C(sp2)H and C(sp3)H Bonds by Using Bidentate Directing Groups

(2013) Guy Rouquet et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Ligand-Accelerated ortho-C–H Alkylation of Arylcarboxylic Acids using Alkyl Boron Reagents

(2013) Peter S. Thuy-Boun et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A robustness screen for the rapid assessment of chemical reactions

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

C–H bond activation enables the rapid construction and late-stage diversification of functional molecules

(2013) Joanna Wencel-Delord et al.   Nature Chemistry

Mild Palladium-Catalyzed C–H Alkylation Using Potassium Alkyltrifluoroborates in Combination with MnF3

(2013) Sharon R. Neufeldt et al.   ORGANIC LETTERS

The Methylation Effect in Medicinal Chemistry

(2011) Eliezer J. Barreiro et al.   CHEMICAL REVIEWS

Divergent C–H Functionalizations Directed by Sulfonamide Pharmacophores: Late-Stage Diversification as a Tool for Drug Discovery

(2011) Hui-Xiong Dai et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY