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

Constructing Iboga Alkaloids via C–H Bond Functionalization: Examination of the Direct and Catalytic Union of Heteroarenes and Isoquinuclidine Alkenes

(2015) Andrew C. Kruegel et al.   JOURNAL OF ORGANIC CHEMISTRY

Atom-Economical Transformation of Diaryliodonium Salts: Tandem C–H and N–H Arylation of Indoles

(2015) Sachin G. Modha 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

Metal-catalysed azidation of tertiary C–H bonds suitable for late-stage functionalization

(2015) Ankit Sharma et al.   NATURE

Late-stage C–H functionalization of complex alkaloids and drug molecules via intermolecular rhodium-carbenoid insertion

(2015) Jing He et al.   Nature Communications

Regioselective Halogenation of 1,4-Benzodiazepinones via CH Activation

(2015) Hajer Abdelkafi et al.   Scientific Reports

C–H Functionalization in the Synthesis of Amino Acids and Peptides

(2014) Anaïs F. M. Noisier et al.   CHEMICAL REVIEWS

Combined Experimental and Computational Investigations of Rhodium- and Ruthenium-Catalyzed C–H Functionalization of Pyrazoles with Alkynes

(2014) Andrés G. Algarra et al.   JOURNAL OF ORGANIC CHEMISTRY

Overriding Ortho–Para Selectivity via a Traceless Directing Group Relay Strategy: The Meta-Selective Arylation of Phenols

(2014) Junfei Luo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Palladium-catalysed C–H activation of aliphatic amines to give strained nitrogen heterocycles

(2014) Andrew McNally et al.   NATURE

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

(2014) M. G. J. Baud et al.   SCIENCE

Palladium-Catalyzedortho-Selective CH Deuteration of Arenes: Evidence for Superior Reactivity of Weakly Coordinated Palladacycles

(2013) Sandy Ma et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Palladium-Catalyzed CHorthoArylation of Benzoic Acids with Diaryliodonium Salts in Water

(2013) Zhiqing Wu et al.   ChemCatChem

Silver Ion Promoted, PdII-Catalyzed Arylation of Arenes with a Free Amine as Directing Group in Aqueous Medium

(2013) Zunjun Liang et al.   CHEMISTRY-A EUROPEAN JOURNAL

Ruthenium(II)-Catalyzed CH Alkenylations of Phenols with Removable Directing Groups

(2013) Wenbo Ma et al.   CHEMISTRY-A EUROPEAN JOURNAL

“On Water”, Phosphine-Free Palladium-Catalyzed Room Temperature CH Arylation of Indoles

(2013) Saidul Islam et al.   CHEMISTRY-A EUROPEAN JOURNAL

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Using Deuterium in Drug Discovery: Leaving the Label in the Drug

(2013) Thomas G. Gant   JOURNAL OF MEDICINAL CHEMISTRY

Radical-Based Regioselective C–H Functionalization of Electron-Deficient Heteroarenes: Scope, Tunability, and Predictability

(2013) Fionn O’Hara et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Palladium-Catalyzed C-2 Selective Arylation of Quinolines

(2013) Xiaoyu Ren et al.   ORGANIC LETTERS

Carboxylate-assisted ruthenium(II)-catalyzed C–H arylations of 5-aryl tetrazoles: step-economical access to Valsartan

(2013) Emelyne Diers et al.   TETRAHEDRON

Synthesis of murrayaquinone A and analogues via ring-closing C–H arylation

(2013) Robin B. Bedford et al.   TETRAHEDRON

Synthesis of novel 2,4-disubstituted 3 H -pyrido[3,2- e ][1,4]diazepin-5-ones and 2,4-disubstituted 3 H -pyrido[2,3- e ][1,4]diazepin-5-ones derivatives via regioselective thionation and nucleophilic substitutions reactions

(2013) Abderrahman El Bouakher et al.   TETRAHEDRON

Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors

(2013) Jin-Jun Liu et al.   ACS Medicinal Chemistry Letters

Ruthenium(II)-Catalyzed Chelation-Assisted Arylation of CH Bonds with Diaryliodonium Salts

(2013) Jordan Sun Ho et al.   Asian Journal of Organic Chemistry

Controlling Site Selectivity in Palladium-Catalyzed C–H Bond Functionalization

(2012) Sharon R. Neufeldt et al.   ACCOUNTS OF CHEMICAL RESEARCH

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

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

Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

(2012) Rachel L. Clark et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library

(2012) Irina Chuckowree et al.   TETRAHEDRON LETTERS

Ruthenium-catalyzed direct oxidative alkenylation of arenes through twofold C–H bond functionalization

(2012) Sergei I. Kozhushkov et al.   Chemical Science

Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

(2011) John Spencer et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

(2011) Panagis Filippakopoulos et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Microwave-assisted synthesis of medium-sized heterocycles

(2011) Abhishek Sharma et al.   CHEMICAL COMMUNICATIONS

Synthesis of 1,2,3-triazole-fused heterocycles viaPd-catalyzed cyclization of 5-iodotriazoles

(2011) Jacqueline M. Schulman et al.   CHEMICAL COMMUNICATIONS

Palladium-Catalyzed Direct Arylation of Heteroaromatic Compounds: Improved Conditions Utilizing Controlled Microwave Heating

(2011) Mostafa Baghbanzadeh et al.   JOURNAL OF ORGANIC CHEMISTRY

Heterocycle Synthesis via Direct C–H/N–H Coupling

(2011) Enrico T. Nadres et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Highly Convergent Total Synthesis of (+)-Lithospermic Acid via a Late-Stage Intermolecular C−H Olefination

(2011) Dong-Hui Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines

(2011) Gabin Mwande-Maguene et al.   NEW JOURNAL OF CHEMISTRY

Changing and challenging times for service crystallography

(2011) Simon J. Coles et al.   Chemical Science

Minisci reactions: Versatile CH-functionalizations for medicinal chemists

(2011) Matthew A. J. Duncton   MedChemComm

Efficient Three-Step One-Pot Synthesis of a Novel 2,3,5-Substituted Pyrazine Library

(2011) Christian Delvare et al.   ACS Combinatorial Science

A Highly Para-Selective Copper(II)-Catalyzed Direct Arylation of Aniline and Phenol Derivatives

(2010) Claire-Lise Ciana et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Palladium-Catalyzed Ligand-Directed C−H Functionalization Reactions

(2010) Thomas W. Lyons et al.   CHEMICAL REVIEWS

1,4-benzodiazepin-2-ones in medicinal chemistry

(2010) John Spencer et al.   Future Medicinal Chemistry

Modulating Reactivity and Diverting Selectivity in Palladium-Catalyzed Heteroaromatic Direct Arylation Through the Use of a Chloride Activating/Blocking Group

(2010) Benoît Liégault et al.   JOURNAL OF ORGANIC CHEMISTRY

Predictable and Site-Selective Functionalization of Poly(hetero)arene Compounds by Palladium Catalysis

(2010) David Lapointe et al.   JOURNAL OF ORGANIC CHEMISTRY

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Diaryliodonium Salts: A Journey from Obscurity to Fame

(2009) Eleanor���A. Merritt et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Application of Daugulis Copper-Catalyzed Direct Arylation to the Synthesis of 5-Aryl Benzotriazepines

(2009) Sirilata Yotphan et al.   ORGANIC LETTERS

Regiospecific One-Pot Synthesis of Diaryliodonium Tetrafluoroborates from Arylboronic Acids and Aryl Iodides

(2008) Marcin Bielawski et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis of a Benzodiazepine-Derived Rhodium NHC Complex by C−H Bond Activation

(2008) Michael W. Gribble et al.   ORGANOMETALLICS

C–H activations on a 1H-1,4-benzodiazepin-2(3H)-one template

(2008) John Spencer et al.   TETRAHEDRON

Fluorine in medicinal chemistry

(2007) Sophie Purser et al.   CHEMICAL SOCIETY REVIEWS