Recent Advances in Methylation: A Guide for Selecting Methylation Reagents

Selective Monomethylation of Amines with Methanol as the C1 Source

(2018) Geunho Choi et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Selective α-Monomethylation by an Amine-Borane/N,N-Dimethylformamide System as the Methyl Source

(2018) Hui-Min Xia et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Benign approach for methyl-esterification of oxygenated organic compounds using TBHP as methylating and oxidizing agent

(2018) Topi Ghosh et al.   APPLIED CATALYSIS B-ENVIRONMENTAL

Improving oral bioavailability of cyclic peptides by N -methylation

(2018) Andreas F.B. Räder et al.   BIOORGANIC & MEDICINAL CHEMISTRY

N terminal N-methylation modulates chiral centre induced helical (CIH) peptides’ biophysical properties

(2018) Wenjun Li et al.   CHEMICAL COMMUNICATIONS

Copper-catalyzed synthesis of α-amino nitriles through methyl transfer from DMF to aromatic amines

(2018) Zaifeng Yuan et al.   CHEMICAL COMMUNICATIONS

Advances in One-Pot Synthesis through Borrowing Hydrogen Catalysis

(2018) Avelino Corma et al.   CHEMICAL REVIEWS

The reactions of dimethyl carbonate and its derivatives

(2018) P. Tundo et al.   GREEN CHEMISTRY

Dimethyl carbonate: a versatile reagent for a sustainable valorization of renewables

(2018) G. Fiorani et al.   GREEN CHEMISTRY

Selective synthesis of mono- and di-methylated amines using methanol and sodium azide as C1 and N1 sources

(2018) Kaushik Chakrabarti et al.   GREEN CHEMISTRY

Decarboxylative reactions with and without light – a comparison

(2018) Johanna Schwarz et al.   GREEN CHEMISTRY

NNN Pincer Ru(II)-Complex-Catalyzed α-Alkylation of Ketones with Alcohols

(2018) Xiao-Niu Cao et al.   JOURNAL OF ORGANIC CHEMISTRY

Organocatalyzed, Visible-Light Photoredox-Mediated, One-Pot Minisci Reaction Using Carboxylic Acids via N-(Acyloxy)phthalimides

(2018) Trevor C. Sherwood et al.   JOURNAL OF ORGANIC CHEMISTRY

gem-Diborylalkanes: recent advances in their preparation, transformation and application

(2018) Rajender Nallagonda et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Inexpensive Radical Methylation and Related Alkylations of Heteroarenes

(2018) Qi Huang et al.   ORGANIC LETTERS

On-Demand Generation and Consumption of Diazomethane in Multistep Continuous Flow Systems

(2018) Hongwei Yang et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Transition-Metal-Free Catalysis for the Reductive ­Functionalization of CO2 with Amines

(2018) Liang-Nian He et al.   SYNLETT

Recent Progress in Methylation of (Hetero)Arenes by Cross-Coupling or C–H Activation

(2018) Yahu Liu et al.   SYNLETT

Selective N -monomethylation of primary anilines with dimethyl carbonate in continuous flow

(2018) Hyowon Seo et al.   TETRAHEDRON

Direct Synthesis of N,N-Dimethylated and β-Methyl N,N-Dimethylated Amines from Nitriles Using Methanol: Experimental and Computational Studies

(2018) Bhaskar Paul et al.   ACS Catalysis

C-Methylation of Alcohols, Ketones, and Indoles with Methanol Using Heterogeneous Platinum Catalysts

(2018) S. M. A. Hakim Siddiki et al.   ACS Catalysis

Highly Selective N-Monomethylanilines Synthesis From Nitroarene and Formaldehyde via Kinetically Excluding of the Thermodynamically Favorable N,N-Dimethylation Reaction

(2018) Hongli Wang et al.   ACS Catalysis

Selective mono N-methylation of anilines with methanol catalyzed by rhenium complexes: An experimental and theoretical study

(2018) Duo Wei et al.   JOURNAL OF CATALYSIS

Recent Progress in Decarboxylative Oxidative Cross-Coupling for Biaryl Synthesis

(2017) Gregory J. P. Perry et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Impact of N -methylation of the substance P 1–7 amide on anti-allodynic effect in mice after peripheral administration

(2017) Anna Skogh et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Metal-free radical C–H methylation of pyrimidinones and pyridinones with dicumyl peroxide

(2017) Pei-Zhi Zhang et al.   GREEN CHEMISTRY

Copper-catalyzed S-methylation of sulfonyl hydrazides with TBHP for the synthesis of methyl sulfones in water

(2017) Yu Yang et al.   GREEN CHEMISTRY

Efficient, selective and sustainable catalysis of carbon dioxide

(2017) Qing-Wen Song et al.   GREEN CHEMISTRY

A highly efficient Suzuki–Miyaura methylation of pyridines leading to the drug pirfenidone and its CD3 version (SD-560)

(2017) Eliezer Falb et al.   GREEN CHEMISTRY

Mono- N -methylation of anilines with methanol catalyzed by a manganese pincer-complex

(2017) Antoine Bruneau-Voisine et al.   JOURNAL OF CATALYSIS

Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry

(2017) Tanaji T. Talele   JOURNAL OF MEDICINAL CHEMISTRY

Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance

(2017) Manuel Lasalle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy

(2017) William McCoull et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Characterization of Urofuranoic Acids: In Vivo Metabolism of 2-(2-Carboxyethyl)-4-methyl-5-propylfuran-3-carboxylic Acid (CMPF) and Effects on in Vitro Insulin Secretion

(2017) Edith Nagy et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Current State of Peptide Drug Discovery: Back to the Future?

(2017) Antoine Henninot et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Synthesis of Trifluoromethyl-sulfonimidamides from Sulfinamides

(2017) Charlotte S. Richards-Taylor et al.   JOURNAL OF ORGANIC CHEMISTRY

Visible-Light-Induced C2 Alkylation of Pyridine N-Oxides

(2017) Wen-Man Zhang et al.   JOURNAL OF ORGANIC CHEMISTRY

Copper-Catalyzed Oxidative Alkylation (Methylation) of Phosphonamides and Phosphinamides Using Dicumyl Peroxide

(2017) Jing Xiao et al.   JOURNAL OF ORGANIC CHEMISTRY

Catalyst-Free and Redox-Neutral Innate Trifluoromethylation and Alkylation of Aromatics Enabled by Light

(2017) Peng Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Autocatalytic backbone N-methylation in a family of ribosomal peptide natural products

(2017) Niels S van der Velden et al.   Nature Chemical Biology

Synthesis, SAR and biological studies of sugar amino acid-based almiramide analogues: N-methylation leads the way

(2017) Dipendu Das et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Copper promoted N-alkylation of sulfoximines with alkylboronic acid under mild conditions

(2017) Surabhi Gupta et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Manganese-Catalyzed Directed Methylation of C(sp2)–H Bonds at 25 °C with High Catalytic Turnover

(2017) Takenari Sato et al.   ORGANIC LETTERS

Tri-Substituted Triazole-Enabled C–H Activation of Benzyl and Aryl Amines by Iron Catalysis

(2017) Zhigao Shen et al.   ORGANIC LETTERS

N-Methylation of Amines with Methanol Catalyzed by a Cp*Ir Complex Bearing a Functional 2,2′-Bibenzimidazole Ligand

(2017) Ran Liang et al.   ORGANIC LETTERS

Copper(II)-Catalyzed Selective Reductive Methylation of Amines with Formic Acid: An Option for Indirect Utilization of CO2

(2017) Chang Qiao et al.   ORGANIC LETTERS

Utilization of MeOH as a C1 Building Block in Tandem Three-Component Coupling Reaction

(2017) Kaushik Chakrabarti et al.   ORGANIC LETTERS

Rhodium(III)-Catalyzed ortho-C–H Alkylation of 2-Arylbenzothiazoles and 2-Arylthiazoles with Potassium Alkyltrifluoroborates

(2017) Qiuping Ding et al.   SYNTHESIS-STUTTGART

Recent Progress on Radical Decarboxylative Alkylation for Csp3–C Bond Formation

(2017) Hongli Bao et al.   SYNTHESIS-STUTTGART

The photochemical alkylation and reduction of heteroarenes

(2017) T. McCallum et al.   Chemical Science

Iron catalyzed methylation and ethylation of vinyl arenes

(2017) Nengbo Zhu et al.   Chemical Science

Metal-free C–H alkylation of heteroarenes with alkyltrifluoroborates: a general protocol for 1°, 2° and 3° alkylation

(2017) Jennifer K. Matsui et al.   Chemical Science

Photoredox radical conjugate addition of dithiane-2-carboxylate promoted by an iridium(iii) phenyl-tetrazole complex: a formal radical methylation of Michael acceptors

(2017) Andrea Gualandi et al.   Chemical Science

Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket

(2017) Hirofumi Nakano et al.   ACS Medicinal Chemistry Letters

Utilization of CO2 as a C1 Building Block for Catalytic Methylation Reactions

(2017) Yuehui Li et al.   ACS Catalysis

CuI promoted sulfenylation of organozinc reagents with arylsulfonyl chlorides

(2017) Ying Fu et al.   RSC Advances

Sustainable and Selective Monomethylation of Anilines by Methanol with Solid Molecular NHC-Ir Catalysts

(2017) Jiangbo Chen et al.   ACS Sustainable Chemistry & Engineering

Supported Palladium Nanoparticle Catalyzed α-Alkylation of Ketones Using Alcohols as Alkylating Agents

(2017) C. Bal Reddy et al.   ACS Sustainable Chemistry & Engineering

Nickel-Catalyzed Directed Benzylation of Ortho C−H Bonds in Aromatic Amides through C−H/C−N Cleavage

(2017) Jiawei Li et al.   Asian Journal of Organic Chemistry

Pd/Ni catalyzed selective N–H/C–H methylation of amides by using peroxides as the methylating reagents via a radical process

(2017) Ze-lin Li et al.   Organic Chemistry Frontiers

Iron Catalyzed Oxidative C(sp3 )-N Cross Coupling of Amides with C(sp3 )-H via a Radical Process

(2017) Ze-lin Li et al.   ChemistrySelect

Simple and Clean Photo-induced Methylation of Heteroarenes with MeOH

(2017) Wenbo Liu et al.   Chem

Phenyltrimethylammonium Salts as Methylation Reagents in the Nickel-Catalyzed Methylation of C−H Bonds

(2016) Takeshi Uemura et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Transition-Metal-Free Regioselective Alkylation of Pyridine N -Oxides Using 1,1-Diborylalkanes as Alkylating Reagents

(2016) Woohyun Jo et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Application of a Palladium-Catalyzed C−H Functionalization/Indolization Method to Syntheses ofcis-Trikentrin A and Herbindole B

(2016) Raul A. Leal et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Nickel-Catalyzed Methylation of Aryl Halides with Deuterated Methyl Iodide

(2016) Lu Hu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Improved Method of S-Alkylation of 2-Mercaptobenzimidazole Derivatives with Trialkylphosphite

(2016) A. El-Kihel et al.   ASIAN JOURNAL OF CHEMISTRY

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT 2C receptor

(2016) Thomas O. Schrader et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Radical trideuteromethylation with deuterated dimethyl sulfoxide in the synthesis of heterocycles and labelled building blocks

(2016) Roberta Caporaso et al.   CHEMICAL COMMUNICATIONS

Carbon–Carbon Bond Forming Reactions via Photogenerated Intermediates

(2016) Davide Ravelli 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

Hitting a Moving Target: How Does anN-Methyl Group Impact Biological Activity?

(2016) Yen Chin Koay et al.   ChemMedChem

Copper(I)-Catalyzed 3-Position Methylation of Coumarins by Using Di-tert-butyl Peroxide as the Methylation Reagents

(2016) Huan Zhuang et al.   CHINESE JOURNAL OF CHEMISTRY

New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors

(2016) Georges Moarbess et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Enantiomerically Pure β-Hydroxy Ketones via β-Keto Weinreb Amides by a Condensation/Asymmetric-Hydrogenation/Acylation Sequence

(2016) Julian Diehl et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists

(2016) Michiyo Mochizuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

(2016) Kevin W. Kuntz et al.   JOURNAL OF MEDICINAL CHEMISTRY

N4-methylation changes the conformation of (3S,6S)-3-alkyl-6-benzylpiperazine-2,5-diones from folded to extended

(2016) Michiyasu Nakao et al.   JOURNAL OF MOLECULAR STRUCTURE

Photoredox Catalysis in Organic Chemistry

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

Radicals: Reactive Intermediates with Translational Potential

(2016) Ming Yan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

N-Methylated α-Amino Acids And Peptides: Synthesis And Biological Activity

(2016) Maria Luisa Di Gioia et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Palladium-catalysed direct C-2 methylation of indoles

(2016) Daoquan Tu et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Functionalization of Azacalixaromatics by Cu(II)-Catalyzed Oxidative Cross-Coupling Reaction between the Arene C–H Bond and Boronic Acids

(2016) Yang Liu et al.   ORGANIC LETTERS

Chemoselective Ketone Synthesis by the Addition of Organometallics to N-Acylazetidines

(2016) Chengwei Liu et al.   ORGANIC LETTERS

Cobalt-Catalyzed Monoselective Ortho-C–H Functionalization of Carboxamides with Organoaluminum Reagent

(2016) Huiqiao Wang et al.   ORGANIC LETTERS

Dicumyl Peroxide as a Methylating Reagent in the Ni-Catalyzed Methylation of Ortho C–H Bonds in Aromatic Amides

(2016) Teruhiko Kubo et al.   ORGANIC LETTERS

N-Methylation of poorly nucleophilic aromatic amines with dimethyl carbonate

(2016) Huidong Yan et al.   RESEARCH ON CHEMICAL INTERMEDIATES

Recent Developments in the Direct Methylation of Electron-­Deficient N-Heteroarenes

(2016) Seung Cho et al.   SYNLETT

Recent Progress on Copper-Mediated Directing-Group-Assisted C(sp2)–H Activation

(2016) Hui-Xiong Dai et al.   SYNTHESIS-STUTTGART

Synthesis of sulfonylated anti -indeno[1,2- d ]pyridazines via oxidative three-component 1,5-enyne-bicyclization

(2016) Bo Jiang et al.   TETRAHEDRON LETTERS

Reductive N-methylation of amines with calcium hydride and Pd/C catalyst

(2016) Carole Guyon et al.   TETRAHEDRON LETTERS

Photoredox-mediated Minisci C–H alkylation of N-heteroarenes using boronic acids and hypervalent iodine

(2016) Guo-Xing Li et al.   Chemical Science

Enantioselective acyl transfer catalysis by a combination of common catalytic motifs and electrostatic interactions

(2016) Hiroki Mandai et al.   Nature Communications

Efficient and selective N-alkylation of amines with alcohols catalysed by manganese pincer complexes

(2016) Saravanakumar Elangovan et al.   Nature Communications

Selective Formylation and Methylation of Amines using Carbon Dioxide and Hydrosilane Catalyzed by Alkali-Metal Carbonates

(2016) Chi Fang et al.   ACS Catalysis

Radical Decarboxylative Functionalizations Enabled by Dual Photoredox Catalysis

(2016) Hanchu Huang et al.   ACS Catalysis

Methylation of aromatic amines and imines using formic acid over a heterogeneous Pt/C catalyst

(2016) Lei Zhu et al.   Catalysis Science & Technology

A general protocol for the reductive N-methylation of amines using dimethyl carbonate and molecular hydrogen: mechanistic insights and kinetic studies

(2016) Jose R. Cabrero-Antonino et al.   Catalysis Science & Technology

Water as Co-Hydrogen Donor in Reductive Aminations

(2016) Zhengang Ke et al.   ACS Sustainable Chemistry & Engineering

N-Alkylation by Hydrogen Autotransfer Reactions

(2016) Xiantao Ma et al.   Topics in Current Chemistry

C-Alkylation by Hydrogen Autotransfer Reactions

(2016) Yasushi Obora   Topics in Current Chemistry

Nickel-Catalyzed Reductive Couplings

(2016) Xuan Wang et al.   Topics in Current Chemistry

Iron-Catalyzed C–H Functionalization Processes

(2016) Gianpiero Cera et al.   Topics in Current Chemistry

N-Methylation as a Strategy for Enhancing the Affinity and Selectivity of RNA-binding Peptides: Application to the HIV-1 Frameshift-Stimulating RNA

(2015) Thomas A. Hilimire et al.   ACS Chemical Biology

Recent Advances in Transition Metal-Catalyzed Methylation Reactions

(2015) Guobing Yan et al.   ADVANCED SYNTHESIS & CATALYSIS

Improving the passive permeability of macrocyclic peptides: Balancing permeability with other physicochemical properties

(2015) Praew Thansandote et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements

(2015) Anthony J. Roecker et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Nickel(II)-Catalyzed Direct Benzylation, Allylation, Alkylation, and Methylation of C–H Bonds in Aromatic Amides Containing an 8-Aminoquinoline Moiety as the Directing Group

(2015) Yoshinori Aihara et al.   BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN

Recent advances in dialkyl carbonates synthesis and applications

(2015) Shouying Huang et al.   CHEMICAL SOCIETY REVIEWS

Enantiomeric Cyclic Peptides with Different Caco-2 Permeability Suggest Carrier-Mediated Transport

(2015) Udaya Kiran Marelli et al.   CHEMISTRY-A EUROPEAN JOURNAL

cis-Peptide Bonds: A Key for Intestinal Permeability of Peptides? 

(2015) Udaya Kiran Marelli et al.   CHEMISTRY-A EUROPEAN JOURNAL

Convenient Reductive Methylation of Amines with Carbonates at Room Temperature

(2015) Yuehui Li et al.   CHEMISTRY-A EUROPEAN JOURNAL

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

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

Transition Metal-free Methylation of Amines with Formaldehyde as the Reductant and Methyl Source

(2015) Nikki Y. T. Man et al.   CHIMIA

N-heterocyclic carbene copper(i) catalysed N-methylation of amines using CO2

(2015) Orlando Santoro et al.   DALTON TRANSACTIONS

Going Out on a Limb: Delineating The Effects of β-Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues

(2015) Andrew T. Bockus et al.   JOURNAL OF MEDICINAL CHEMISTRY

Aerobic Copper-Catalyzed O-Methylation with Methylboronic Acid

(2015) Clare E. Jacobson et al.   JOURNAL OF ORGANIC CHEMISTRY

Unexpected Retroaldol-Aldol Reaction during O-Alkylation of Hydroxylated Vince Lactam Derivatives

(2015) Christoffer Bengtsson et al.   JOURNAL OF ORGANIC CHEMISTRY

DMF Dimethyl Acetal as Carbon Source for α-Methylation of Ketones: A Hydrogenation–Hydrogenolysis Strategy of Enaminones

(2015) Ashwini Borah et al.   JOURNAL OF ORGANIC CHEMISTRY

Lewis acid catalysed methylation ofN-(9H-fluoren-9-yl)methanesulfonyl (Fms) protected lipophilicα-amino acid methyl esters

(2015) Antonella Leggio et al.   JOURNAL OF PEPTIDE SCIENCE

Iron-Catalyzed Directed C(sp2)–H and C(sp3)–H Functionalization with Trimethylaluminum

(2015) Rui Shang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Alcohols as alkylating agents in heteroarene C–H functionalization

(2015) Jian Jin et al.   NATURE

Copper-catalyzed N-methylation/ethylation of sulfoximines

(2015) Fan Teng et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Synthesis and stability of cyclic α-hydrogen nitroxides

(2015) Hila Toledo et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Metal-free methylation of a pyridine N-oxide C–H bond by using peroxides

(2015) Gang Li et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

N-Methylation of Amines with Methanol at Room Temperature

(2015) Vasily N. Tsarev et al.   ORGANIC LETTERS

Rh(III)-Catalyzed C–H Alkylation of Arenes Using Alkylboron Reagents

(2015) He Wang et al.   ORGANIC LETTERS

Dimethyl sulfite a potential agent for methylation

(2015) Rim Mouselmani et al.   TETRAHEDRON

A practical, chemoselective approach to O-methylation of carboxylic acids with dimethyl malonate

(2015) Jincheng Mao et al.   TETRAHEDRON

The use of dialkyl acetals in the N-alkylation of 8-oxoadenosine and guanosine. Mechanistic studies and rate determination

(2015) Tewoderos Ayele et al.   TETRAHEDRON LETTERS

Aryl/heteroaryl pentafluorobenzenesulfonates (ArOPFBs): new electrophilic coupling partners for room temperature Suzuki–Miyaura cross-coupling reactions

(2015) Jayan T. Joseph et al.   TETRAHEDRON LETTERS

The effect of N-methylation on transition state mimetic inhibitors of the Plasmodium protease, plasmepsin V

(2015) Michelle Gazdik et al.   MedChemComm

Insights into the impact of N- and O-methylation on aqueous solubility and lipophilicity using matched molecular pair analysis

(2015) T. J. Ritchie et al.   MedChemComm

Efficient Ruthenium-Catalyzed N-Methylation of Amines Using Methanol

(2015) Tuan Thanh Dang et al.   ACS Catalysis

The Stille Reaction, 38 Years Later

(2015) Carlos Cordovilla et al.   ACS Catalysis

Reusable, Highly Active Heterogeneous Palladium Catalyst by Convenient Self-Encapsulation Cross-Linking Polymerization for Multiple CarbonCarbon Cross-Coupling Reactions at ppm to ppb Palladium Loadings

(2014) Zhongmin Dong et al.   ADVANCED SYNTHESIS & CATALYSIS

Copper-Catalyzed Intermolecular Trifluoromethylazidation of Alkenes: Convenient Access to CF3-Containing Alkyl Azides

(2014) Fei Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Metal-Free Catalyst for the Chemoselective Methylation of Amines Using Carbon Dioxide as a Carbon Source

(2014) Shoubhik Das et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Late-Stage Functionalization of Biologically Active Heterocycles Through Photoredox Catalysis

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

Synthesis of IB-01212 by multiple N-methylations of peptide bonds

(2014) Ryota Nabika et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dimethylsulfoxide as an N-Methylation Reagent for Amines and Aromatic Nitro Compounds

(2014) Benjamin N. Atkinson et al.   ChemCatChem

Rhodium-Catalyzed Decarbonylative Direct C2-Arylation of Indoles with Aryl Carboxylic Acids

(2014) Lingjuan Zhang et al.   ChemCatChem

N-Methyl and peptoid scans of an autoinducing peptide reveal new structural features required for inhibition and activation of AgrC quorum sensing receptors in Staphylococcus aureus

(2014) Yftah Tal-Gan et al.   CHEMICAL COMMUNICATIONS

Iridium-catalyzed selective α-methylation of ketones with methanol

(2014) Shinji Ogawa et al.   CHEMICAL COMMUNICATIONS

Methylation of secondary amines with dialkyl carbonates and hydrosilanes catalysed by iron complexes

(2014) Jianxia Zheng et al.   CHEMICAL COMMUNICATIONS

General Catalytic Methylation of Amines with Formic Acid under Mild Reaction Conditions

(2014) Iván Sorribes et al.   CHEMISTRY-A EUROPEAN JOURNAL

Copper-Catalyzed Decarboxylative Methylation of Aromatic Carboxylic Acids with PhI(OAc)2

(2014) Yuyu Jiang et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

An Environmentally Friendly Method forN-Methylation of 5-Substituted 1H-Tetrazoles with a Green Methylating Reagent: Dimethyl Carbonate

(2014) Aming Xie et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Synthesis and Biological Evaluation of 2-Aryliminopyrrolidines as Selective Ligands for I1 Imidazoline Receptors: Discovery of New Sympatho-Inhibitory Hypotensive Agents with Potential Beneficial Effects in Metabolic Syndrome

(2014) Vincent Gasparik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lead Optimization of 1,4-Azaindoles as Antimycobacterial Agents

(2014) Pravin S. Shirude et al.   JOURNAL OF MEDICINAL CHEMISTRY

tert-Butyl Peroxybenzoate-Promoted α-Methylation of 1,3-Dicarbonyl Compounds

(2014) Songjin Guo et al.   JOURNAL OF ORGANIC CHEMISTRY

Pd-Catalyzed Monoselective ortho-C–H Alkylation of N-Quinolyl Benzamides: Evidence for Stereoretentive Coupling of Secondary Alkyl Iodides

(2014) Shu-Yu Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Stereospecific Cross-Coupling Reactions of Aryl-Substituted Tetrahydrofurans, Tetrahydropyrans, and Lactones

(2014) Emily J. Tollefson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Iron-Catalyzed Coupling of Aryl Sulfamates and Aryl/Vinyl Tosylates with Aryl Grignards

(2014) Toolika Agrawal et al.   ORGANIC LETTERS

Development of the Direct Suzuki–Miyaura Cross-Coupling of Primary B-Alkyl MIDA-boronates and Aryl Bromides

(2014) Jeffrey D. St. Denis et al.   ORGANIC LETTERS

Nickel-Catalyzed Reductive Methylation of Alkyl Halides and Acid Chlorides with Methyl p-Tosylate

(2014) Zhuye Liang et al.   ORGANIC LETTERS

Dual Roles of Sulfonyl Hydrazides: A Three-Component Reaction To Construct Fully Substituted Pyrazoles Using TBAI/TBHP

(2014) Jie Zhang et al.   ORGANIC LETTERS

Single-electron transmetalation in organoboron cross-coupling by photoredox/nickel dual catalysis

(2014) J. C. Tellis et al.   SCIENCE

Unprecedented C-Methylation at the 2-Position of 2-Carboxy-4-Chromanones – A Case Study with the Corey–Chaykovsky Reagent

(2014) Bishwajit Ganguly et al.   SYNLETT

Iron-catalyzed decarboxylative methylation of α,β-unsaturated acids under ligand-free conditions

(2014) Guangwei Rong et al.   TETRAHEDRON

Microwave-mediated synthesis of N-methyliminodiacetic acid (MIDA) boronates

(2014) Adam J. Close et al.   TETRAHEDRON

Acid- and isobutylene-free synthesis of t-butyl ethers by in situ formation of 2-t-butoxy-1-methylpyridinium triflate

(2014) Anna E. Salvati et al.   TETRAHEDRON LETTERS

Dihydropyrrolo[2,3-d]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts

(2014) Manabu Watanabe et al.   ACS Medicinal Chemistry Letters

Recent Advances in α-Alkylation Reactions using Alcohols with Hydrogen Borrowing Methodologies

(2014) Yasushi Obora   ACS Catalysis

Magnesium oxide as a heterogeneous and recyclable base for the N-methylation of indole and O-methylation of phenol using dimethyl carbonate as a green methylating agent

(2014) Sandip T. Gadge et al.   RSC Advances

Upgrading of Biobased Lactones with Dialkylcarbonates

(2014) Alessio Caretto et al.   ACS Sustainable Chemistry & Engineering

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

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

A General Method for N-Methylation of Amines and Nitro Compounds with Dimethylsulfoxide

(2013) Xue Jiang et al.   CHEMISTRY-A EUROPEAN JOURNAL

Effect of Ester to Amide orN-Methylamide Substitution on Bacterial Membrane Depolarization and Antibacterial Activity of Novel Cyclic Lipopeptides

(2013) Nina Bionda et al.   ChemMedChem

Fluorenylmethoxycarbonyl-N-methylamino Acids Synthesized in a Flow Tube-in-Tube Reactor with a Liquid-Liquid Semipermeable Membrane

(2013) Annette E. Buba et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Catalytic Methyl Transfer from Dimethylcarbonate to Carboxylic Acids

(2013) Yuan Ji et al.   JOURNAL OF ORGANIC CHEMISTRY

Iron Halide-Mediated Regio- and Stereoselective Halosulfonylation of Terminal Alkynes with Sulfonylhydrazides: Synthesis of (E)-β-Chloro and Bromo Vinylsulfones

(2013) Xiaoqing Li et al.   JOURNAL OF ORGANIC CHEMISTRY

Total Synthesis of Ecteinascidin 743

(2013) Fumiki Kawagishi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Functional-Group-Tolerant, Nickel-Catalyzed Cross-Coupling Reaction for Enantioselective Construction of Tertiary Methyl-Bearing Stereocenters

(2013) Hanna M. Wisniewska et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tetrabutylammonium iodide catalyzed allylic sulfonylation of Baylis–Hillman acetates with sulfonylhydrazides in water

(2013) Xiaoqing Li et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Selective, On-Resin N-Methylation of Peptide N-Trifluoroacetamides

(2013) Rushia A. Turner et al.   ORGANIC LETTERS

DMF as Carbon Source: Rh-Catalyzed α-Methylation of Ketones

(2013) Yang Li et al.   ORGANIC LETTERS

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

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

Selective Methylation of NH-Containing Heterocycles and Sulfonamides Using N,N-Dimethylformamide Dimethylacetal Based on Calculated pKa Measurements

(2013) Gary Fairley et al.   SYNLETT

Nickel-catalyzed cross-coupling of unactivated alkyl halides using bis(pinacolato)diboron as reductant

(2013) Hailiang Xu et al.   Chemical Science

Dialkyl phosphite as a highly selective mono-N-alkylating agent using indium triflate under microwave irradiation

(2013) Shrishnu Kumar Kundu et al.   RSC Advances

Evidence for an Intermediate in the Methylation of CB11H12−with Methyl Triflate: Comparison of Electrophilic Substitution in Cage Boranes and in Arenes

(2013) Jiří Kaleta et al.   ChemPlusChem

Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints

(2012) Jonathan E. Bock et al.   ACS Chemical Biology

N-Methylation of Peptides and Proteins: An Important Element for Modulating Biological Functions

(2012) Jayanta Chatterjee et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity

(2012) Matthew E. Voss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity

(2012) Jean-Philippe Surivet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Future of Peptide-based Drugs

(2012) David J. Craik et al.   Chemical Biology & Drug Design

Synthesis and biological evaluation of novel (−)-cercosporamide derivatives as potent selective PPARγ modulators

(2012) Akihiro Furukawa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Methylation using dimethylcarbonate catalysed by ionic liquids under continuous flow conditions

(2012) Toma N. Glasnov et al.   GREEN CHEMISTRY

Methyl Effects on Protein–Ligand Binding

(2012) Cheryl S. Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections

(2012) Justin I. Montgomery et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorous Oxime Palladacycle: A Precatalyst for Carbon–Carbon Coupling Reactions in Aqueous and Organic Medium

(2012) Woen Susanto et al.   JOURNAL OF ORGANIC CHEMISTRY

Cross-Coupling Reaction with Lithium Methyltriolborate

(2012) Yasunori Yamamoto et al.   MOLECULES

Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives

(2012) Kate M. Clapham et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Ketone Formation via Mild Nickel-Catalyzed Reductive Coupling of Alkyl Halides with Aryl Acid Chlorides

(2012) Fan Wu et al.   ORGANIC LETTERS

Traceless Directing Group for Stereospecific Nickel-Catalyzed Alkyl−Alkyl Cross-Coupling Reactions

(2012) Margaret A. Greene et al.   ORGANIC LETTERS

Regioselective Synthesis of Trialkylpyrazines via Nickel-Catalyzed Negishi Cross-Coupling of Pyrazine Triflate

(2012) Kee-In Lee et al.   SYNTHESIS-STUTTGART

General and efficient method for direct N-monomethylation of aromatic primary amines with methanol

(2012) Feng Li et al.   RSC Advances

Farewell to the HSAB Treatment of Ambident Reactivity

(2011) Herbert Mayr et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Methylation Effect in Medicinal Chemistry

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

Room-Temperature Ionic Liquids: Solvents for Synthesis and Catalysis. 2

(2011) Jason P. Hallett et al.   CHEMICAL REVIEWS

Synthesis and evaluation of the substrate activity of C-6 substituted purine ribosides with E. coli purine nucleoside phosphorylase: Palladium mediated cross-coupling of organozinc halides with 6-chloropurine nucleosides

(2011) Abdalla E.A. Hassan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905)

(2011) Matthew O. Duffey et al.   JOURNAL OF MEDICINAL CHEMISTRY

9-Substituted 6,6-Dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as Highly Selective and Potent Anaplastic Lymphoma Kinase Inhibitors

(2011) Kazutomo Kinoshita et al.   JOURNAL OF MEDICINAL CHEMISTRY

On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds

(2011) Tina R White et al.   Nature Chemical Biology

Nickel-catalyzed Negishi cross-couplings of 6-chloropurines with organozinc halides at room temperature

(2011) Dong-Chao Wang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Solid-Phase Synthesis of NMe-IB-01212, a Highly N-Methylated Cyclic Peptide

(2011) Eleonora Marcucci et al.   ORGANIC LETTERS

Ionic Liquids—Promoted S-Methylation of Thiols Utilizing Dimethyl Carbonate

(2011) Jiangang Xie et al.   PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS

N-Alkylation of N-arylsulfonyl-α-amino acid methyl esters by trialkyloxonium tetrafluoroborates

(2011) Rosaria De Marco et al.   TETRAHEDRON

Synthesis of hexahydro[2]benzopyrano[4,3-c]pyridines as serotonin 5-HT2C receptor agonists via intramolecular hetero Diels–Alder reactions

(2011) Yasuko Kiyoi et al.   TETRAHEDRON LETTERS

Synthesis of hexahydro[2]benzopyrano[3,4-c]pyrroles as serotonin 5-HT2C receptor agonists via intramolecular hetero Diels–Alder reactions

(2011) Takao Kiyoi et al.   TETRAHEDRON LETTERS

Minisci reactions: Versatile CH-functionalizations for medicinal chemists

(2011) Matthew A. J. Duncton   MedChemComm

Efficient and chemoselective alkylation of amines/amino acids using alcohols as alkylating reagents under mild conditions

(2010) Chu-Pei Xu et al.   CHEMICAL COMMUNICATIONS

Pd0-Catalyzed carbonylation of 1,1-dichloro-1-alkenes, a new selective access to Z-α-chloroacrylates

(2010) Martin Arthuis et al.   CHEMICAL COMMUNICATIONS

Organic Carbonates as Solvents in Synthesis and Catalysis

(2010) Benjamin Schäffner et al.   CHEMICAL REVIEWS

Chemical Modifications Designed to Improve Peptide Stability: Incorporation of Non-Natural Amino Acids, Pseudo-Peptide Bonds, and Cyclization

(2010) Luca Gentilucci et al.   CURRENT PHARMACEUTICAL DESIGN

An Efficient Preparation ofN-Methyl-α-amino Acids fromN-Nosyl-α-amino Acid Phenacyl Esters

(2010) Antonella Leggio et al.   JOURNAL OF ORGANIC CHEMISTRY

Zinc-Catalyzed Reduction of Amides: Unprecedented Selectivity and Functional Group Tolerance

(2010) Shoubhik Das et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of a Second-Generation, Highly Efficient Manufacturing Route for the HIV Integrase Inhibitor Raltegravir Potassium

(2010) Guy R. Humphrey et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Dimethyl carbonate as a modern green reagent and solvent

(2010) F Aricò et al.   RUSSIAN CHEMICAL REVIEWS

Safe and Efficient Reductive Methylation of Primary and Secondary Amines UsingN-Methylpyrrolidine Zinc Borohydride

(2010) Heshmatollah Alinezhad et al.   SYNTHETIC COMMUNICATIONS

Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents

(2009) Saleem Ahmad et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

DNA methylation by dimethyl sulfoxide and methionine sulfoxide triggered by hydroxyl radical and implications for epigenetic modifications

(2009) Kazuaki Kawai et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Mitsunobu and Related Reactions: Advances and Applications

(2009) K. C. Kumara Swamy et al.   CHEMICAL REVIEWS

Methylation of 2′-Deoxyguanosine by a Free Radical Mechanism

(2009) Conor Crean et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Highly Selective Monomethylation of Primary Amines Through Host−Guest Product Sequestration

(2009) Roger M. Yebeutchou et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Dendritic Polystyrene with Hydroxyl-Functionalized Branch Points by Convergent Living Anionic Polymerization

(2009) Jack T. Bender et al.   MACROMOLECULES

Selective Monomethylation of Anilines by Cu(OAc)2-Promoted Cross-Coupling with MeB(OH)2

(2009) Israel González et al.   ORGANIC LETTERS

A Versatile Catalyst System for Suzuki−Miyaura Cross-Coupling Reactions of C(sp2)-Tosylates and Mesylates

(2009) Brijesh Bhayana et al.   ORGANIC LETTERS

GreenN-Methylation of Electron Deficient Pyrroles with Dimethylcarbonate

(2009) Michael L. Laurila et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Synthesis of 1,1-Dioxobenzo[b]thiophene-2-ylmethyloxycarbonyl (Bsmoc) Protected N-Methyl Amino Acids by Reduction of Bsmoc-5-Oxazolidinones and Their Use in Peptide Synthesis

(2009) Chennakrishnareddy Gundala et al.   PROTEIN AND PEPTIDE LETTERS

N-Methylation of Peptides: A New Perspective in Medicinal Chemistry

(2008) Jayanta Chatterjee et al.   ACCOUNTS OF CHEMICAL RESEARCH

A preparation of N-Fmoc-N-methyl-α-amino acids and N-nosyl-N-methyl-α-amino acids

(2008) Maria Luisa Di Gioia et al.   AMINO ACIDS

Improving Oral Bioavailability of Peptides by Multiple N-Methylation: Somatostatin Analogues

(2008) Eric Biron et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

N-Methyl Scanning Mutagenesis Generates Protease-Resistant G Protein Ligands with Improved Affinity and Selectivity

(2008) Stephen V. Fiacco et al.   CHEMBIOCHEM

Fully reversible guest exchange in tetraphosphonate cavitand complexes probed by fluorescence spectroscopy

(2008) Elisa Biavardi et al.   CHEMICAL COMMUNICATIONS

An Environmentally Benign Access to Dimethylated 1,6-Dihydropyrimidines Using Dimethyl Carbonate as Methylating Agent under Microwave

(2008) Xi-Cun WANG et al.   CHINESE JOURNAL OF CHEMISTRY

Peptide Backbone Modifications

(2008) Uli Kazmaier et al.   CURRENT ORGANIC CHEMISTRY

Green chemistry metrics: a comparative evaluation of dimethyl carbonate, methyl iodide, dimethyl sulfate and methanol as methylating agents

(2008) Maurizio Selva et al.   GREEN CHEMISTRY

Microwave-Assisted Efficient Methylation of Alkyl and Arenesulfonamides with Trimethylsulfoxonium Iodide and KOH

(2008) Sarika Malik et al.   SYNTHETIC COMMUNICATIONS