Late-stage C–H functionalization offers new opportunities in drug discovery

Synthetic and Mechanistic Implications of Chlorine Photoelimination in Nickel/Photoredox C(sp3)–H Cross-Coupling

(2021) Stavros K. Kariofillis et al.   ACCOUNTS OF CHEMICAL RESEARCH

Bayesian reaction optimization as a tool for chemical synthesis

(2021) Benjamin J. Shields et al.   NATURE

Organic reactivity from mechanism to machine learning

(2021) Kjell Jorner et al.   Nature Reviews Chemistry

Bidentate Directing Groups: An Efficient Tool in C–H Bond Functionalization Chemistry for the Expedient Construction of C–C Bonds

(2020) Supriya Rej et al.   CHEMICAL REVIEWS

Differentiation and functionalization of remote C–H bonds in adjacent positions

(2020) Hang Shi et al.   Nature Chemistry

Pushing the boundaries of C–H bond functionalization chemistry using flow technology

(2020) Sebastian Govaerts et al.   Journal of Flow Chemistry

Engineering new catalytic activities in enzymes

(2020) Kai Chen et al.   Nature Catalysis

Copper-catalysed benzylic C–H coupling with alcohols via radical relay enabled by redox buffering

(2020) Huayou Hu et al.   Nature Catalysis

Metal-free photoredox-catalysed formal C–H/C–H coupling of arenes enabled by interrupted Pummerer activation

(2020) Miles H. Aukland et al.   Nature Catalysis

Emerging strategies for expanding the toolbox of enzymes in biocatalysis

(2020) Braddock A. Sandoval et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Biocatalysis in drug discovery and development

(2020) Anna Fryszkowska et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Achieving Site-Selectivity for C–H Activation Processes Based on Distance and Geometry: A Carpenter’s Approach

(2020) Guangrong Meng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines

(2020) Patrick S. Fier et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enzymatic Primary Amination of Benzylic and Allylic C(sp3)–H Bonds

(2020) Zhi-Jun Jia et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Late-stage oxidative C(sp3)–H methylation

(2020) Kaibo Feng et al.   NATURE

The merger of decatungstate and copper catalysis to enable aliphatic C(sp3)–H trifluoromethylation

(2020) Patrick J. Sarver et al.   Nature Chemistry

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

(2020) Stig D. Friis et al.   Nature Chemistry

Diverse functionalization of strong alkyl C–H bonds by undirected borylation

(2020) Raphael Oeschger et al.   SCIENCE

Late-Stage Diversification of Natural Products

(2020) Benke Hong et al.   ACS Central Science

When metal-catalyzed C–H functionalization meets visible-light photocatalysis

(2020) Lucas Guillemard et al.   Beilstein Journal of Organic Chemistry

Photoenzymatic enantioselective intermolecular radical hydroalkylation

(2020) Xiaoqiang Huang et al.   NATURE

Harder, better, faster

(2020) Danielle Schultz et al.   Nature Chemistry

Late-Stage Functionalization

(2020) Jonas Börgel et al.   Chem

Broadening the scope of biocatalytic C–C bond formation

(2020) Lara E. Zetzsche et al.   Nature Reviews Chemistry

From desktop to benchtop with automated computational workflows for computer-aided design in asymmetric catalysis

(2020) Mihai Burai Patrascu et al.   Nature Catalysis

Molecular Machine Learning: The Future of Synthetic Chemistry?

(2020) Philipp M. Pflüger et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Redox‐Neutral TEMPO Catalysis: Direct Radical (Hetero)Aryl C−H Di‐ and Trifluoromethoxylation

(2020) Johnny W. Lee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Regioselective C−H Functionalization of Heteroarene N ‐Oxides Enabled by a Traceless Nucleophile

(2020) Gangadhar Rao Mathi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Direct Conversion of N-Alkylamines to N-Propargylamines through C–H Activation Promoted by Lewis Acid/Organocopper Catalysis: Application to Late-Stage Functionalization of Bioactive Molecules

(2020) Jessica Z. Chan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Modular and Stereoselective Synthesis of C-Aryl Glycosides via Catellani Reaction

(2020) Weiwei Lv et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Functionalization of Pyridinium Derivatives with 1,4-Dihydropyridines Enabled by Photoinduced Charge Transfer

(2020) Inwon Kim et al.   ORGANIC LETTERS

Design and Implementation of a Catalytic Electron Donor–Acceptor Complex Platform for Radical Trifluoromethylation and Alkylation

(2020) Edward J. McClain et al.   ACS Catalysis

Site-Selective Functionalization of Methionine Residues via Photoredox Catalysis

(2020) Junyong Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Photoelectrochemical C-H Alkylation of Heteroarenes with Organotrifluoroborates

(2019) Hong Yan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Prediction of higher-selectivity catalysts by computer-driven workflow and machine learning

(2019) Andrew F. Zahrt et al.   SCIENCE

Electrooxidative Amination of sp2 C–H Bonds: Coupling of Amines with Aryl Amides via Copper Catalysis

(2019) Subban Kathiravan et al.   ORGANIC LETTERS

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

(2019) Florian Berger et al.   NATURE

Recent Advances in Minisci-Type Reactions

(2019) Rupert S. J. Proctor et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Overview of Recent Strategic Advances in Medicinal Chemistry

(2019) Gaochan Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Construction of Natural-Product-Like Cyclophane-Braced Peptide Macrocycles via sp3 C–H Arylation

(2019) Bo Li et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Practical and regioselective amination of arenes using alkyl amines

(2019) Alessandro Ruffoni et al.   Nature Chemistry

The Evolution of High-Throughput Experimentation in Pharmaceutical Development, and Perspectives on the Future

(2019) Steven M Mennen et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Photo-Biocatalysis: Biotransformations in the Presence of Light

(2019) Luca Schmermund et al.   ACS Catalysis

Photoexcitation of flavoenzymes enables a stereoselective radical cyclization

(2019) Kyle F. Biegasiewicz et al.   SCIENCE

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

(2019) Michael Moir et al.   Expert Opinion on Drug Discovery

Nickellaelectro-Catalyzed C-H Alkoxylation with Secondary Alcohols: Oxidation-Induced Reductive Elimination at Nickel(III)

(2019) Shou-Kun Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cobalt(III)-Catalyzed C−H Amidation of Dehydroalanine for the Site-Selective Structural Diversification of Thiostrepton

(2019) Ryan J. Scamp et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Evolved Aliphatic Halogenases Enable Regiocomplementary C−H Functionalization of a Pharmaceutically Relevant Compound

(2019) Takahiro Hayashi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis, Structure, and Reactivity of 5-(Aryl)dibenzothiophenium Triflates

(2019) Kevin Kafuta et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Late-Stage Functionalization of Histidine in Unprotected Peptides

(2019) Anaïs F. M. Noisier et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Histidine-Specific Peptide Modification via Visible-Light-Promoted C–H Alkylation

(2019) Xiaoping Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Photoredox catalysis with aryl sulfonium salts enables site-selective late-stage fluorination

(2019) Jiakun Li et al.   Nature Chemistry

Ruthenium(II)‐Catalyzed Hydrogen Isotope Exchange of Pharmaceutical Drugs by C−H Deuteration and C−H Tritiation

(2019) Valentin Müller et al.   ChemCatChem

Electrophotocatalytic Undirected C−H Trifluoromethylations of (Het)Arenes

(2019) Youai Qiu et al.   CHEMISTRY-A EUROPEAN JOURNAL

Catalytic C(sp3)–H bond activation in tertiary alkylamines

(2019) Jesus Rodrigalvarez et al.   Nature Chemistry

Late-Stage Diversification by Selectivity Switch in meta-C–H Activation: Evidence for Singlet Stabilization

(2019) Korkit Korvorapun et al.   ACS Catalysis

DMSO-catalysed late-stage chlorination of (hetero)arenes

(2019) Song Song et al.   Nature Catalysis

Catalytic C−H Trifluoromethoxylation of Arenes and Heteroarenes

(2018) Weijia Zheng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

BODIPY Peptide Labeling by Late-Stage C(sp3 )−H Activation

(2018) Wei Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Site-Selective δ-C(sp3 )−H Alkylation of Amino Acids and Peptides with Maleimides via a Six-Membered Palladacycle

(2018) Bei-Bei Zhan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Late-Stage Peptide Diversification by Position-Selective C-H Activation

(2018) Wei Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Radical Trifluoromethoxylation of Arenes Triggered by a Visible-Light-Mediated N-O Redox Fragmentation

(2018) Antonio Togni et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Electrochemical C−H Amination by Cobalt Catalysis in a Renewable Solvent

(2018) Nicolas Sauermann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Application of Q2MM to predictions in stereoselective synthesis

(2018) Anthony R. Rosales et al.   CHEMICAL COMMUNICATIONS

Formation and Cleavage of C–C Bonds by Enzymatic Oxidation–Reduction Reactions

(2018) F. Peter Guengerich et al.   CHEMICAL REVIEWS

Catalyst- and Reagent-free Electrochemical Azole C-H Amination

(2018) Youai Qiu et al.   CHEMISTRY-A EUROPEAN JOURNAL

Computational prediction of chemical reactions: current status and outlook

(2018) Ola Engkvist et al.   DRUG DISCOVERY TODAY

Site-Selective Switching Strategies to Functionalize Polyazines

(2018) Ryan D. Dolewski et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

A general strategy for synthesis of cyclophane-braced peptide macrocycles via palladium-catalysed intramolecular sp3 C−H arylation

(2018) Xuekai Zhang et al.   Nature Chemistry

Cyclometallated ruthenium catalyst enables late-stage directed arylation of pharmaceuticals

(2018) Marco Simonetti et al.   Nature Chemistry

Complementary site-selectivity in arene functionalization enabled by overcoming the ortho constraint in palladium/norbornene catalysis

(2018) Jianchun Wang et al.   Nature Chemistry

Organic synthesis provides opportunities to transform drug discovery

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

Visible Light-Mediated Decarboxylative Alkylation of Pharmaceutically Relevant Heterocycles

(2018) Alexandra C. Sun et al.   ORGANIC LETTERS

Radical Chlorodifluoromethylation: Providing a Motif for (Hetero)arene Diversification

(2018) Rory C. McAtee et al.   ORGANIC LETTERS

Catalytic enantioselective Minisci-type addition to heteroarenes

(2018) Rupert S. J. Proctor et al.   SCIENCE

β C–H di-halogenation via iterative hydrogen atom transfer

(2018) Ethan A. Wappes et al.   Chemical Science

Transient Directing Groups for Transformative C–H Activation by Synergistic Metal Catalysis

(2018) Parthasarathy Gandeepan et al.   Chem

Radical Retrosynthesis

(2018) Joel M. Smith et al.   ACCOUNTS OF CHEMICAL RESEARCH

Redox-Active Reagents for Photocatalytic Generation of the OCF3 Radical and (Hetero)Aryl C−H Trifluoromethoxylation

(2018) Weijia Zheng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2018) Carlo Sambiagio et al.   CHEMICAL SOCIETY REVIEWS

Aliphatic C—H Oxidations for Late-Stage Functionalization

(2018) M. Christina White et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Electrochemical Aminoxyl-Mediated α-Cyanation of Secondary Piperidines for Pharmaceutical Building Block Diversification

(2018) Alastair J. J. Lennox et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nanoscale synthesis and affinity ranking

(2018) Nathan J. Gesmundo et al.   NATURE

Expanding the medicinal chemistry synthetic toolbox

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

Late-Stage Diversification by Manganese-Catalyzed C-H Activation: Access to Acyclic, Hybrid and Stapled Peptides

(2018) Nikolaos Kaplaneris et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent Advances in Alkyl Carbon-Carbon Bond Formation by Nickel/Photoredox Cross-Coupling

(2018) Gary Molander et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Pyridyl Radical Cation for C−H Amination of Arenes

(2018) Simon L. Rössler et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Divergent Late-Stage (Hetero)aryl C−H Amination by the Pyridinium Radical Cation

(2018) Won Seok Ham et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Advances in Lead Generation

(2018) Joerg Holenz et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

Site-Selective C–H Functionalization of (Hetero)Arenes via Transient, Non-symmetric Iodanes

(2018) Stacy C. Fosu et al.   Chem

Enzymatic C H functionalizations for natural product synthesis

(2018) Fuzhuo Li et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Selective C H bond functionalization with engineered heme proteins: new tools to generate complexity

(2018) Ruijie K Zhang et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

Electrochemical Cobalt-Catalyzed C–H Oxygenation at Room Temperature

(2017) Nicolas Sauermann et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Late-Stage C–H Alkylation of Heterocycles and 1,4-Quinones via Oxidative Homolysis of 1,4-Dihydropyridines

(2017) Álvaro Gutiérrez-Bonet et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chemoenzymatic Total Synthesis and Structural Diversification of Tylactone-Based Macrolide Antibiotics through Late-Stage Polyketide Assembly, Tailoring, and C—H Functionalization

(2017) Andrew N. Lowell et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Total Synthesis of Nigelladine A via Late-Stage C–H Oxidation Enabled by an Engineered P450 Enzyme

(2017) Steven A. Loskot 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

Enantioselective, intermolecular benzylic C–H amination catalysed by an engineered iron-haem enzyme

(2017) Christopher K. Prier et al.   Nature Chemistry

Snap deconvolution: An informatics approach to high-throughput discovery of catalytic reactions

(2017) Konstantin Troshin et al.   SCIENCE

Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds

(2017) Yong Yao Loh et al.   SCIENCE

4-Selective Pyridine Functionalization Reactions via Heterocyclic Phosphonium Salts

(2017) Andrew McNally et al.   SYNLETT

Synthesis of bioactive and stabilized cyclic peptides by macrocyclization using C(sp3)–H activation

(2017) Jian Tang et al.   Chemical Science

Selective C–O bond formation via a photocatalytic radical coupling strategy: access to perfluoroalkoxylated (ORF) arenes and heteroarenes

(2017) Johnny W. Lee et al.   Chemical Science

Mechanochemical Rhodium(III)-Catalyzed C–H Bond Amidation of Arenes with Dioxazolones under Solventless Conditions in a Ball Mill

(2017) Gary N. Hermann et al.   ACS Catalysis

On the design of complex drug candidate syntheses in the pharmaceutical industry

(2017) Martin D. Eastgate et al.   Nature Reviews Chemistry

The merger of transition metal and photocatalysis

(2017) Jack Twilton et al.   Nature Reviews Chemistry

Elucidation of Mechanisms and Selectivities of Metal-Catalyzed Reactions using Quantum Chemical Methodology

(2016) Stefano Santoro et al.   ACCOUNTS OF CHEMICAL RESEARCH

Single-Electron Transmetalation via Photoredox/Nickel Dual Catalysis: Unlocking a New Paradigm for sp3–sp2 Cross-Coupling

(2016) John C. Tellis et al.   ACCOUNTS OF CHEMICAL RESEARCH

Overcoming the Limitations of C−H Activation with Strongly Coordinating N-Heterocycles by Cobalt Catalysis

(2016) Hui Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

C–H activation reactions as useful tools for medicinal chemists

(2016) Eduardo J.E. Caro-Diaz et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Applications of Continuous-Flow Photochemistry in Organic Synthesis, Material Science, and Water Treatment

(2016) Dario Cambié et al.   CHEMICAL REVIEWS

Organic Photoredox Catalysis

(2016) Nathan A. Romero et al.   CHEMICAL REVIEWS

Direct (Hetero)arylation Polymerization: Simplicity for Conjugated Polymer Synthesis

(2016) Jean-Rémi Pouliot 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 Catalysis in Organic Chemistry

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

Selective Functionalization of Pyridines via Heterocyclic Phosphonium Salts

(2016) Michael C. Hilton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Palladium-catalysed transannular C–H functionalization of alicyclic amines

(2016) Joseph J. Topczewski et al.   NATURE

Iron-catalysed tritiation of pharmaceuticals

(2016) Renyuan Pony Yu et al.   NATURE

Charge-transfer-directed radical substitution enables para-selective C–H functionalization

(2016) Gregory B. Boursalian et al.   Nature Chemistry

Mechanistic studies on intramolecular C–H trifluoromethoxylation of (hetero)arenes via OCF3-migration

(2016) Katarzyna N. Lee et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Visible Light Photocatalysis: Applications and New Disconnections in the Synthesis of Pharmaceutical Agents

(2016) James J. Douglas et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Access to a new class of synthetic building blocks via trifluoromethoxylation of pyridines and pyrimidines

(2016) Pengju Feng et al.   Chemical Science

Late Stage Azidation of Complex Molecules

(2016) Rashad R. Karimov et al.   ACS Central Science

The Molecular Basis of Sustainability

(2016) Paul T. Anastas et al.   Chem

Expanding the toolbox of organic chemists: directed evolution of P450 monooxygenases as catalysts in regio- and stereoselective oxidative hydroxylation

(2015) Gheorghe-Doru Roiban et al.   CHEMICAL COMMUNICATIONS

Drug Oxidation by Cytochrome P450BM3: Metabolite Synthesis and Discovering New P450 Reaction Types

(2015) Xinkun Ren et al.   CHEMISTRY-A EUROPEAN JOURNAL

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis 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

N-Acyl Amino Acid Ligands for Ruthenium(II)-Catalyzed meta-C–H tert-Alkylation with Removable Auxiliaries

(2015) Jie Li et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mechanistic Studies on the Rh(III)-Mediated Amido Transfer Process Leading to Robust C–H Amination with a New Type of Amidating Reagent

(2015) Yoonsu Park 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

Ligand-enabled meta-C–H activation using a transient mediator

(2015) Xiao-Chen Wang et al.   NATURE

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

(2015) Ankit Sharma et al.   NATURE

Palladium-catalysed norbornene-mediated C–H functionalization of arenes

(2015) Juntao Ye et al.   Nature Chemistry

Efficient and Practical Oxidative Bromination and Iodination of Arenes and Heteroarenes with DMSO and Hydrogen Halide: A Mild Protocol for Late-Stage Functionalization

(2015) Song Song et al.   ORGANIC LETTERS

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

(2015) Jing He et al.   Nature Communications

New peptide architectures through C–H activation stapling between tryptophan–phenylalanine/tyrosine residues

(2015) Lorena Mendive-Tapia et al.   Nature Communications

Late-Stage Functionalization of Biologically Active Heterocycles Through Photoredox Catalysis

(2014) Daniel A. DiRocco et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

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

Functional group directed C–H borylation

(2014) A. Ros et al.   CHEMICAL SOCIETY REVIEWS

Palau’chlor: A Practical and Reactive Chlorinating Reagent

(2014) Rodrigo A. Rodriguez et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis and Late-Stage Functionalization of Complex Molecules through C–H Fluorination and Nucleophilic Aromatic Substitution

(2014) Patrick S. Fier et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Site-Selective C(sp3)–H Functionalization of Di-, Tri-, and Tetrapeptides at the N-Terminus

(2014) Wei Gong et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Late Stage Benzylic C–H Fluorination with [18F]Fluoride for PET Imaging

(2014) Xiongyi Huang 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

Contemporary screening approaches to reaction discovery and development

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

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

(2014) A. Buitrago Santanilla et al.   SCIENCE

Discovery of Potent Parthenolide-Based Antileukemic Agents Enabled by Late-Stage P450-Mediated C—H Functionalization

(2013) Joshua N. Kolev et al.   ACS Chemical Biology

Visible Light Photoredox Catalysis with Transition Metal Complexes: Applications in Organic Synthesis

(2013) Christopher K. Prier et al.   CHEMICAL REVIEWS

meta-Selective C–H Bond Alkylation with Secondary Alkyl Halides

(2013) Nora Hofmann et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Ortho- and Para-Selective Ruthenium-Catalyzed C(sp2)–H Oxygenations of Phenol Derivatives

(2013) Weiping Liu et al.   ORGANIC LETTERS

Selective C-H Fluorination of Pyridines and Diazines Inspired by a Classic Amination Reaction

(2013) P. S. Fier et al.   SCIENCE

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

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

Rhodium-Catalyzed Intermolecular Amidation of Arenes with Sulfonyl Azides via Chelation-Assisted C–H Bond Activation

(2012) Ji Young Kim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Controlled Oxidation of Remote sp3 C–H Bonds in Artemisinin via P450 Catalysts with Fine-Tuned Regio- and Stereoselectivity

(2012) Kaidong Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Pd(II)-Catalyzed Regioselective 2-Alkylation of Indoles via a Norbornene-Mediated C–H Activation: Mechanism and Applications

(2012) Lei Jiao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Activation of remote meta-C–H bonds assisted by an end-on template

(2012) Dasheng Leow et al.   NATURE

Practical and innate carbon–hydrogen functionalization of heterocycles

(2012) Yuta Fujiwara et al.   NATURE

Sterically Controlled Iodination of Arenes via Iridium-Catalyzed C–H Borylation

(2012) Benjamin M. Partridge et al.   ORGANIC LETTERS

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

(2012) W. Liu et al.   SCIENCE

Innate and Guided C–H Functionalization Logic

(2011) Tobias Brückl et al.   ACCOUNTS OF CHEMICAL RESEARCH

C–H functionalization logic in total synthesis

(2011) Will R. Gutekunst et al.   CHEMICAL SOCIETY REVIEWS

Recent developments in natural product synthesis using metal-catalysed C–H bond functionalisation

(2011) Lindsay McMurray et al.   CHEMICAL SOCIETY 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

Regio- and stereoselectivity of P450-catalysed hydroxylation of steroids controlled by laboratory evolution

(2011) Sabrina Kille et al.   Nature Chemistry

Innate C-H trifluoromethylation of heterocycles

(2011) Y. Ji et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Minisci reactions: Versatile CH-functionalizations for medicinal chemists

(2011) Matthew A. J. Duncton   MedChemComm

Enzymatic functionalization of carbon–hydrogen bonds

(2010) Jared C. Lewis et al.   CHEMICAL SOCIETY REVIEWS

The development and use of novel iridium complexes as catalysts for ortho-directed hydrogen isotope exchange reactions

(2010) Göran N. Nilsson et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Direct C−H Arylation of Electron-Deficient Heterocycles with Arylboronic Acids

(2010) Ian B. Seiple et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Transition-Metal-Catalyzed Direct Arylation of (Hetero)Arenes by CH Bond Cleavage

(2009) Lutz Ackermann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Panel of Cytochrome P450 BM3 Variants to Produce Drug Metabolites and Diversify Lead Compounds

(2009) Andrew M. Sawayama et al.   CHEMISTRY-A EUROPEAN JOURNAL

Catalytic Sequential Reactions Involving Palladacycle-Directed Aryl Coupling Steps

(2008) Marta Catellani et al.   ACCOUNTS OF CHEMICAL RESEARCH

Biologically inspired oxidation catalysis

(2008) Lawrence Que et al.   NATURE

Chemo-enzymatic fluorination of unactivated organic compounds

(2008) Andrea Rentmeister et al.   Nature Chemical Biology