Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals

Recent Developments in Ruthenium-Catalyzed C–H Arylation: Array of Mechanistic Manifolds

(2017) Pradeep Nareddy et al.   ACS Catalysis

Late Stage CH Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines

(2016) Raysa Khan et al.   ADVANCED SYNTHESIS & CATALYSIS

Evaluating New Chemistry to Drive Molecular Discovery: Fit for Purpose?

(2016) Daniel J. Foley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

Ru-Catalyzed C–H Arylation of Fluoroarenes with Aryl Halides

(2016) Marco Simonetti et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Microwave-assisted regioselective direct C–H arylation of thiazole derivatives leading to increased σ1 receptor affinity

(2016) Artur Kokornaczyk et al.   MedChemComm

Understanding Our Love Affair with p-Chlorophenyl: Present Day Implications from Historical Biases of Reagent Selection

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

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

Pd(ii)-catalyzed, controllable C–H mono-/diarylation of aryl tetrazoles: concise synthesis of Losartan

(2015) Yan-Jun Ding et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

What does the aromatic ring number mean for drug design?

(2014) Simon E Ward et al.   Expert Opinion on Drug Discovery

Beyond C, H, O, and N! Analysis of the Elemental Composition of U.S. FDA Approved Drug Architectures

(2014) Brandon R. Smith 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

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

Overcoming the limitations of directed C–H functionalizations of heterocycles

(2014) Yue-Jin Liu et al.   NATURE

An organic cation as a silver(i) analogue for the arylation of sp2 and sp3 C–H bonds with iodoarenes

(2014) Carlos Arroniz et al.   Chemical Science

Non-directed allylic C–H acetoxylation in the presence of Lewis basic heterocycles

(2014) Hasnain A. Malik et al.   Chemical Science

Improvement of σ1 receptor affinity by late-stage C–H-bond arylation of spirocyclic lactones

(2013) Christina Meyer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, Structure, and Antibiotic Activity of Aryl-Substituted LpxC Inhibitors

(2013) Xiaofei Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Data-Mining for Sulfur and Fluorine: An Evaluation of Pharmaceuticals To Reveal Opportunities for Drug Design and Discovery

(2013) Elizabeth A. Ilardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry

(2012) Alan Nadin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

CH Bond Functionalization: Emerging Synthetic Tools for Natural Products and Pharmaceuticals

(2012) Junichiro Yamaguchi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Expanding medicinal chemistry space

(2012) Andy Barker et al.   DRUG DISCOVERY TODAY

Carboxylate-Assisted Transition-Metal-Catalyzed C−H Bond Functionalizations: Mechanism and Scope

(2011) Lutz Ackermann   CHEMICAL REVIEWS

The Medicinal Chemist’s Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates

(2011) Stephen D. Roughley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Autocatalysis for C–H Bond Activation by Ruthenium(II) Complexes in Catalytic Arylation of Functional Arenes

(2011) Emmanuel Ferrer Flegeau et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

CH Bond Functionalization in Water Catalyzed by Carboxylato Ruthenium(II) Systems

(2010) Percia B. Arockiam et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Factors Determining the Selection of Organic Reactions by Medicinal Chemists and the Use of These Reactions in Arrays (Small Focused Libraries)

(2010) Tony W. J. Cooper et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The impact of aromatic ring count on compound developability: further insights by examining carbo- and hetero-aromatic and -aliphatic ring types

(2010) Timothy J. Ritchie et al.   DRUG DISCOVERY TODAY

Mechanistic Insight into Direct Arylations with Ruthenium(II) Carboxylate Catalysts

(2010) Lutz Ackermann et al.   ORGANIC LETTERS

The impact of aromatic ring count on compound developability – are too many aromatic rings a liability in drug design?

(2009) Timothy J. Ritchie et al.   DRUG DISCOVERY TODAY

Direct Arylation of Arene C−H Bonds by Cooperative Action of NHCarbene−Ruthenium(II) Catalyst and Carbonate via Proton Abstraction Mechanism

(2008) Ismail Özdemir et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Assisted Ruthenium-Catalyzed C−H Bond Activation: Carboxylic Acids as Cocatalysts for Generally Applicable Direct Arylations in Apolar Solvents

(2008) Lutz Ackermann et al.   ORGANIC LETTERS