Exploring Electrochemical C(sp3)–H Oxidation for the Late-Stage Methylation of Complex Molecules

A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment

(2021) Alessia Balestrini et al.   JOURNAL OF EXPERIMENTAL MEDICINE

N-Ammonium Ylide Mediators for Electrochemical C–H Oxidation

(2021) Masato Saito et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

C(sp3)–H methylation enabled by peroxide photosensitization and Ni-mediated radical coupling

(2021) Aristidis Vasilopoulos et al.   SCIENCE

C( sp 3 )−C( sp 3 ) Bond Formation via Electrochemical Alkoxylation and Subsequent Lewis Acid Promoted Reactions

(2021) Enol López et al.   ADVANCED SYNTHESIS & CATALYSIS

C–H Amination via Electrophotocatalytic Ritter-type Reaction

(2021) Tao Shen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Copper catalyzed late-stage C(sp3)-H functionalization of nitrogen heterocycles

(2021) Zhe Chang et al.   Nature Communications

Unlocking the Potential of High-Throughput Experimentation for Electrochemistry with a Standardized Microscale Reactor

(2021) Jonas Rein et al.   ACS Central Science

An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19

(2021) Dafydd R. Owen et al.   SCIENCE

Essential Medicinal Chemistry of Essential Medicines

(2020) Marta Serafini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Late-stage oxidative C(sp3)–H methylation

(2020) Kaibo Feng et al.   NATURE

Electrochemical Ruthenium-Catalyzed C–H Hydroxylation of Amine Derivatives in Aqueous Acid

(2020) Sophia G. Robinson et al.   ORGANIC LETTERS

Site-selective electrooxidation of methylarenes to aromatic acetals

(2020) Peng Xiong et al.   Nature Communications

Electrode Materials in Modern Organic Electrochemistry

(2020) David Heard et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Electrochemical N-Demethylation of 14-Hydroxy Morphinans: Sustainable Access to Opioid Antagonists

(2020) Gabriel Glotz et al.   ORGANIC LETTERS

Manganese-Catalyzed Oxidative Azidation of C(sp3)–H Bonds under Electrophotocatalytic Conditions

(2020) Linbin Niu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Harnessing Alkylpyridinium Salts as Electrophiles in Deaminative Alkyl–Alkyl Cross-Couplings

(2019) Shane Plunkett et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Late-Stage Functionalization of Peptides and Cyclopeptides Using Organozinc Reagents

(2019) Marcel Leroux et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

α-Functionalization of Cyclic Secondary Amines: Lewis Acid Promoted Addition of Organometallics to Transient Imines

(2019) Anirudra Paul et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Fluorinated Alcohols: Magic Reaction Medium and Promoters for Organic Synthesis

(2019) Xiao‐De An et al.   CHEMICAL RECORD

Sulfa drug analogs: new classes of N-sulfonyl aminated azines and their biological and preclinical importance in medicinal chemistry (2000–2018)

(2019) Galal H. Elgemeie et al.   MEDICINAL CHEMISTRY RESEARCH

Metal- and Reagent-Free Dehydrogenative Formal Benzyl-Aryl Cross-Coupling by Anodic Activation in 1,1,1,3,3,3-Hexafluoropropan-2-ol

(2018) Yasushi Imada et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Electrochemical Functional-Group-Tolerant Shono-type Oxidation of Cyclic Carbamates Enabled by Aminoxyl Mediators

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

Stereoselective nucleophilic addition reactions to cyclic N-acyliminium ions using the indirect cation pool method: Elucidation of stereoselectivity by spectroscopic conformational analysis and DFT calculations

(2018) Koichi Mitsudo et al.   Beilstein Journal of Organic Chemistry

Anodic benzylic C(sp3)–H amination: unified access to pyrrolidines and piperidines

(2018) Sebastian Herold et al.   GREEN CHEMISTRY

Discovery of a Potent (4R,5S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling

(2018) Huifen Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

C–H Bond Functionalization of Tetrahydropyridopyrimidines and Other Related Hetereocycles

(2017) Zhanling Cheng et al.   JOURNAL OF ORGANIC CHEMISTRY

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

(2017) Chip Le et al.   NATURE

Hexafluoroisopropanol as a highly versatile solvent

(2017) Ignacio Colomer et al.   Nature Reviews Chemistry

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

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

Enantioselective amine α-functionalization via palladium-catalysed C–H arylation of thioamides

(2016) Pankaj Jain et al.   Nature Chemistry

A general alkyl-alkyl cross-coupling enabled by redox-active esters and alkylzinc reagents

(2016) T. Qin et al.   SCIENCE

Practical Electrochemical Anodic Oxidation of Polycyclic Lactams for Late Stage Functionalization

(2015) Kevin J. Frankowski et al.   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

Platinum-Catalyzed, Terminal-Selective C(sp3)–H Oxidation of Aliphatic Amines

(2015) Melissa Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Concerted proton-coupled electron transfer from a metal-hydride complex

(2015) Marc Bourrez et al.   Nature Chemistry

The Shono-type electroorganic oxidation of unfunctionalised amides. Carbon–carbon bond formation via electrogeneratedN-acyliminium ions

(2014) Alan M Jones et al.   Beilstein Journal of Organic 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

Expedient Preparation of Nazlinine and a Small Library of Indole Alkaloids Using Flow Electrochemistry as an Enabling Technology

(2014) Mikhail A. Kabeshov et al.   ORGANIC LETTERS

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

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

TRP Channels and Pain

(2013) David Julius   Annual Review of Cell and Developmental Biology

Discovery of [(2R,5R)-5-{[(5-Fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): A Dual Orexin Receptor Antagonist with Potent Sleep-Promoting Properties

(2012) Paul J. Coleman et al.   ChemMedChem

The Methylation Effect in Medicinal Chemistry

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

General Method for the Expedient Synthesis of Salt-Free Diorganozinc Reagents Using Zinc Methoxide

(2008) Alexandre Côté et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY