The Deuterated “Magic Methyl” Group: A Guide to Site‐Selective Trideuteromethyl Incorporation and Labeling by Using CD 3 Reagents

Pd-Catalyzed ipso,meta-Dimethylation of ortho-Substituted Iodoarenes via a Base-Controlled C–H Activation Cascade with Dimethyl Carbonate as the Methyl Source

(2021) Zhuo Wu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Iridium-catalyzed C−H methylation and d3-methylation of benzoic acids with application to late-stage functionalizations

(2021) Erik Weis et al.   iScience

1,1-Ethenediol: The Long Elusive Enol of Acetic Acid

(2020) Artur Mardyukov et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Palladium-Catalyzed Direct α-Arylation of Arylacetonitriles with Aryl Tosylates and Mesylates

(2020) On Ying Yuen et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Synthesis of 2-Amino-1,3-dienes from Propargyl Carbonates via Palladium-Catalyzed Carbon–Nitrogen Bond Formation

(2020) Calvin Q. O’Broin et al.   ORGANIC LETTERS

Electrophotocatalytic Decarboxylative C−H Functionalization of Heteroarenes

(2020) Xiao‐Li Lai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Room‐temperature Palladium‐Catalyzed Deuterogenolysis of Carbon Oxygen Bonds towards Deuterated Pharmaceuticals

(2020) Wei Ou et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery

(2020) Robert W. Pipal et al.   NATURE

Applications of deuterium in medicinal chemistry

(2019) Tracey Pirali et al.   JOURNAL OF MEDICINAL CHEMISTRY

Trideuteromethylation Enabled by a Sulfoxonium Metathesis Reaction

(2019) Zuyuan Shen et al.   ORGANIC LETTERS

Highly Chemo-, Regio- and E/Z-Selective Intermolecular Heck-Type Dearomative [2 + 2 + 1] Spiroannulation of Alkyl Bromoarenes with Internal Alkynes

(2019) Xingrong Liao et al.   ORGANIC LETTERS

Rhodium-Catalyzed Selective C–H Trideuteromethylation of Indole at C7 Position Using Acetic-d6 Anhydride

(2019) Xiaowei Han et al.   JOURNAL OF ORGANIC CHEMISTRY

Hydroalkylation of Olefins To Form Quaternary Carbons

(2019) Samantha A. Green et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Iridium-Catalyzed α-Methylation of α-Aryl Esters Using Methanol as the C1 Source

(2019) Yuya Tsukamoto et al.   ORGANIC LETTERS

Iron-Catalyzed Tandem Three-Component Alkylation: Access to α-Methylated Substituted Ketones

(2019) Léo Bettoni et al.   ORGANIC LETTERS

The Alkylation and Reduction of Heteroarenes with Alcohols Using Photoredox Catalyzed Hydrogen Atom Transfer via Chlorine Atom Generation

(2019) Montserrat Zidan et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

A primer of deuterium in drug design

(2019) Sarah Cargnin et al.   Future Medicinal Chemistry

Palladacycle-Phosphine Catalyzed Methylation of Amines and Ketones Using Methanol

(2019) Ramesh Mamidala et al.   JOURNAL OF ORGANIC CHEMISTRY

Modular Dual-Tasked C–H Methylation via the Catellani Strategy

(2019) Qianwen Gao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

One-Pot Conversion of Allylic Alcohols to α-Methyl Ketones via Iron-Catalyzed Isomerization–Methylation

(2019) Daniel E. Latham et al.   ORGANIC LETTERS

Iron-Catalyzed Borrowing Hydrogen β-C(sp3)-Methylation of Alcohols

(2019) Kurt Polidano et al.   ACS Catalysis

Manganese(I)-Catalyzed β-Methylation of Alcohols Using Methanol as C1 Source

(2019) Akash Kaithal et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

On the mechanism of the Ruthenium‐catalyzed β‐methylation of alcohols with methanol

(2019) Markus Hoelscher et al.   ChemCatChem

Iron-Catalyzed β-Alkylation of Alcohols

(2019) Léo Bettoni et al.   ORGANIC LETTERS

C–H Nickelation of Naphthyl Phosphinites: Electronic and Steric Limitations, Regioselectivity, and Tandem C–P Functionalization

(2019) Loïc P. Mangin et al.   ORGANOMETALLICS

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

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

Advances in One-Pot Synthesis through Borrowing Hydrogen Catalysis

(2018) Avelino Corma et al.   CHEMICAL REVIEWS

Catalytic (de)hydrogenation promoted by non-precious metals – Co, Fe and Mn: recent advances in an emerging field

(2018) Georgy A. Filonenko et al.   CHEMICAL SOCIETY REVIEWS

DMSO as a Switchable Alkylating Agent in Heteroarene C−H Functionalization

(2018) R. Aleyda Garza-Sanchez et al.   CHEMISTRY-A EUROPEAN JOURNAL

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

(2018) G. Fiorani et al.   GREEN CHEMISTRY

Primary deuterium kinetic isotope effects prolong drug release and polymer biodegradation in a drug delivery system

(2018) Brian R. Hearn et al.   JOURNAL OF CONTROLLED RELEASE

Modular ipso/ortho Difunctionalization of Aryl Bromides via Palladium/Norbornene Cooperative Catalysis

(2018) Zhe Dong et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Copper-Catalyzed Methylboration of Alkenes

(2018) Bin Chen et al.   ORGANIC LETTERS

Nickel and Nucleophilic Cobalt-Catalyzed Trideuteriomethylation of Aryl Halides Using Trideuteriomethyl p-Toluenesulfonate

(2018) Kimihiro Komeyama et al.   ORGANIC LETTERS

Synthesis and photophysical properties of deuteration of pirfenidone

(2018) Qiuju Yin et al.   SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

One-Pot Highly Regioselective Synthesis of Indole-Fused Pyridazino[4,5-b][1,4]benzoxazepin-4(3H)-ones by a Smiles Rearrangement

(2018) Fangdong Hu et al.   SYNLETT

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

Mechanistic Study of the Nickel-Catalyzed α,β-Coupling of Saturated Ketones

(2018) Xin Zhang et al.   ACS Catalysis

Iron-Catalyzed Methylation Using the Borrowing Hydrogen Approach

(2018) Kurt Polidano et al.   ACS Catalysis

Cobalt-catalyzed directed ortho-methylation of arenes with methyl tosylate

(2018) Qiao Sun et al.   Organic Chemistry Frontiers

ortho-Amino group functionalized 2,2′-bipyridine based Ru(ii) complex catalysed alkylation of secondary alcohols, nitriles and amines using alcohols

(2018) Bivas Chandra Roy et al.   Organic Chemistry Frontiers

Iron-Mediated Azidomethylation or Azidotrideuteromethylation of Active Alkenes with Azidotrimethylsilane and Dimethyl Sulfoxide

(2018) Rui Zhang et al.   ADVANCED SYNTHESIS & CATALYSIS

Development of an Alkyne-de Mayo Reaction for the Synthesis of Medium-Sized Carbacycles and Cyclohepta[b]indoles

(2018) Martin Hiersemann et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals

(2018) Edward M. Russak et al.   ANNALS OF PHARMACOTHERAPY

Methyl-containing pharmaceuticals: Methylation in drug design

(2018) Shaoyi Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Palladium-Catalyzed Intermolecular [4+1] Spiroannulation by C(sp3 )−H Activation and Naphthol Dearomatization

(2018) Bojun Tan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Catalytic C1  Alkylation with Methanol and Isotope-Labeled Methanol

(2018) Jan Sklyaruk et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Recent Advances in Methylation: A Guide for Selecting Methylation Reagents

(2018) Yantao Chen   CHEMISTRY-A EUROPEAN JOURNAL

Combination of PhI(OAc)2 and 2-Nitropropane as the Source of Methyl Radical in Room-Temperature Metal-Free Oxidative Decarboxylation/Cyclization: Construction of 6-Methyl Phenanthridines and 1-Methyl Isoquinolines

(2018) Shi-Chao Lu et al.   JOURNAL OF ORGANIC CHEMISTRY

Metallaphotoredox-Catalyzed Cross-Electrophile Csp3–Csp3 Coupling of Aliphatic Bromides

(2018) Russell T. Smith et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Cooperative Palladium/Lewis Acid-Catalyzed Transfer Hydrocyanation of Alkenes and Alkynes Using 1-Methylcyclohexa-2,5-diene-1-carbonitrile

(2018) Anup Bhunia et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Deuterated drugs; updates and obviousness analysis

(2017) Graham S. Timmins   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Isotope labelling by reduction of nitriles: Application to the synthesis of isotopologues of tolmetin and celecoxib

(2017) Kate Ellis-Sawyer et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

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

(2017) Tanaji T. Talele   JOURNAL OF MEDICINAL CHEMISTRY

Mechanistic Investigations of the Iron(III)-Catalyzed Carbonyl-Olefin Metathesis Reaction

(2017) Jacob R. Ludwig et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

First deuterated drug approved

(2017) Charles Schmidt   NATURE BIOTECHNOLOGY

5-Formylcytosine to cytosine conversion by C–C bond cleavage in vivo

(2017) Katharina Iwan et al.   Nature Chemical Biology

Visible-light-induced and iron-catalyzed methylation of N-arylacrylamides with dimethyl sulphoxide: a convenient access to 3-ethyl-3-methyl oxindoles

(2017) Zuguang Xie et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

(2017) Kaushik Chakrabarti et al.   ORGANIC LETTERS

The photochemical alkylation and reduction of heteroarenes

(2017) T. McCallum et al.   Chemical Science

Free-radical initiated cascade methylation or trideuteromethylation of isocyanides with dimethyl sulfoxides

(2017) Rui Zhang et al.   RSC Advances

Simple and Clean Photo-induced Methylation of Heteroarenes with MeOH

(2017) Wenbo Liu et al.   Chem

Nickel-Catalyzed Methylation of Aryl Halides with Deuterated Methyl Iodide

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

Unexplored Reactivity of N-Alkyl Unsaturated Imines: A Simple Procedure for Producing Optically Active 1,3-Diamines via a Stereocontrolled Formal [4+2] and [4+2+2] Iminocycloaddition

(2016) Ambara R. Pradipta et al.   BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN

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

(2016) Roberta Caporaso et al.   CHEMICAL COMMUNICATIONS

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

(2016) Yen Chin Koay et al.   ChemMedChem

Deuterium medicinal chemistry comes of age

(2016) Roger D Tung   Future Medicinal Chemistry

Synthesis of stable isotope labeled D9-Mabuterol, D9-Bambuterol, and D9-Cimbuterol

(2016) Yahui Tu et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

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

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

Copper-Catalyzed Intramolecular Benzylic C–H Amination for the Synthesis of Isoindolinones

(2016) Chiaki Yamamoto et al.   JOURNAL OF ORGANIC CHEMISTRY

Stereoselective synthesis of 1β,25-Dihydroxyvitamin D 3 and its 26,27-hexadeuterated derivative

(2016) Julian Loureiro et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Deuterated drugs draw heavier backing

(2016) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

I2-Mediated 2H-indazole synthesis via halogen-bond-assisted benzyl C–H functionalization

(2016) Xiangli Yi et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Hydrogen-Transfer-Mediated Direct β-Alkylation of Aryl-1,8-naphthyridines with Alcohols under Transition Metal Catalyst Free Conditions

(2016) Biao Xiong et al.   ORGANIC LETTERS

Palladium-catalyzed Catellani-type couplings using methylating reagents for the synthesis of highly substituted ortho-methyl-arenes and heteroarenes

(2016) Jonathan E. Wilson   TETRAHEDRON LETTERS

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

Synthesis and Stereochemical Assignment of Crypto-Optically Active2H6-Neopentane

(2015) Ahmad Masarwa et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Step into an eco-Compatible Future: Iron- and Cobalt-catalyzed Borrowing Hydrogen Transformation

(2015) Adrien Quintard et al.   ChemSusChem

Steric Effects on the Primary Isotope Dependence of Secondary Kinetic Isotope Effects in Hydride Transfer Reactions in Solution: Caused by the Isotopically Different Tunneling Ready State Conformations?

(2015) Binita Maharjan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Hydromethylation of Unactivated Olefins

(2015) Hai T. Dao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Stereospecific Nickel-Catalyzed Cross-Coupling Reactions of Benzylic Ethers with Isotopically-Labeled Grignard Reagents

(2015) David D. Dawson et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

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

Iridium-catalyzed methylation of indoles and pyrroles using methanol as feedstock

(2015) Shu-Jie Chen et al.   RSC Advances

Palladium-catalyzed alkylation of unactivated C(sp3)–H bonds with primary alkyl iodides at room temperature: facile synthesis of β-alkyl α-amino acids

(2015) B. Wang et al.   Organic Chemistry Frontiers

Catalytic Methylation of CH Bonds Using CO2and H2

(2014) Yuehui Li et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enantioselective Synthesis of Chiral Isotopomers of 1-Alkanols by a ZACA-Cu-Catalyzed Cross-Coupling Protocol

(2014) Shiqing Xu et al.   CHEMISTRY-A EUROPEAN JOURNAL

Deuterated drugs: where are we now?

(2014) Graham S Timmins   EXPERT OPINION ON THERAPEUTIC PATENTS

Efficient, scalable and economical preparation of tris(deuterium)- and13C-labelledN-methyl-N-nitroso-p-toluenesulfonamide (Diazald®) and their conversion to labelled diazomethane

(2014) Samuel W. J. Shields et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

δ-Deuterium Isotope Effects as Probes for Transition-State Structures of Isoprenoid Substrates

(2014) Seoung-ryoung Choi et al.   JOURNAL OF ORGANIC CHEMISTRY

An In Situ Directing Group Strategy for Chiral Anion Phase-Transfer Fluorination of Allylic Alcohols

(2014) Weiwei Zi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

C–H Methylation of Heteroarenes Inspired by Radical SAM Methyl Transferase

(2014) Jinghan Gui et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Ligand-Promoted Alkylation of C(sp3)–H and C(sp2)–H Bonds

(2014) Ru-Yi Zhu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Selective Isotope Labelling of Leucine Residues by Using α-Ketoacid Precursor Compounds

(2013) Roman J. Lichtenecker et al.   CHEMBIOCHEM

Synthesis of isotopically labeled epothilones

(2013) Thota Ganesh et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

A facile synthesis of 5,5-dideutero-4-dimethyl(phenyl)silyl-6-undecyl-tetrahydropyran-2-one as a deuterium labeled synthon for (−)-tetrahydrolipstatin and (+)-δ-hexadecanolide

(2013) Sandip J. Wagh et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Optimization of Chloronitrobenzamides (CNBs) as Therapeutic Leads for Human African Trypanosomiasis (HAT)

(2013) Jong Yeon Hwang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Dual PLD1/2 and PLD2 Selective Inhibitors from a Common 1,3,8-Triazaspiro[4.5]decane Core: Discovery of ML298 and ML299 That Decrease Invasive Migration in U87-MG Glioblastoma Cells

(2013) Matthew C. O’Reilly 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

Palladium-Catalyzed Methylation of Alkynyl C(sp)–H Bonds with Dimethyl Sulfonium Ylides

(2013) Yan-Yun Liu et al.   JOURNAL OF ORGANIC CHEMISTRY

Palladium-Catalyzed Picolinamide-Directed Alkylation of Unactivated C(sp3)–H Bonds with Alkyl Iodides

(2013) Shu-Yu Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A frustrated-Lewis-pair approach to catalytic reduction of alkynes to cis-alkenes

(2013) Konstantin Chernichenko et al.   Nature Chemistry

Heavy drugs draw heavy interest from pharma backers

(2013) Alla Katsnelson   NATURE MEDICINE

Palladium-Catalyzed CH Oxidation of Isoquinoline N-Oxides: Selective Alkylation with Dialkyl Sulfoxides and Halogenation with Dihalo sulfoxides

(2012) Bo Yao et al.   ADVANCED SYNTHESIS & CATALYSIS

Stereoselection in the Corey-Bakshi-Shibata Reduction: Insight from Kinetic Isotope Effects and Transition-Structure Modeling

(2012) Hui Zhu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Stereochemical Course and Mechanism of the IspH Reaction

(2012) Christian A. Citron et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Potent and Selective S1P1 Antagonist with Efficacy in Experimental Autoimmune Encephalomyelitis

(2012) Jean Quancard et al.   CHEMISTRY & 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

Cyclochiral resorcin[4]arenes as effective enantioselectors in the gas phase

(2012) Caterina Fraschetti et al.   JOURNAL OF MASS SPECTROMETRY

Methyl Effects on Protein–Ligand Binding

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

Finding the sweet spot: the role of nature and nurture in medicinal chemistry

(2012) Michael M. Hann et al.   NATURE REVIEWS DRUG DISCOVERY

Improved assignment of vibrational modes in sum-frequency spectra in the CH stretch region for surface-bound C18 alkylsilanes

(2012) Arthur D. Quast et al.   VIBRATIONAL SPECTROSCOPY

Escape from Flatland 2: complexity and promiscuity

(2012) Frank Lovering   MedChemComm

“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

(2011) Michael R. Wood et al.   BIOCHEMISTRY

The Methylation Effect in Medicinal Chemistry

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

Synthesis of deuterium-labeled d3-androstenone and d3-skatole for boar taint analysis

(2011) Jochen Fischer et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Discovery and SAR of Methylated Tetrahydropyranyl Derivatives as Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase (ICMT)

(2011) Weston R. Judd et al.   JOURNAL OF MEDICINAL CHEMISTRY

1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis

(2011) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biphenyl-Substituted Oxazolidinones as Cholesteryl Ester Transfer Protein Inhibitors: Modifications of the Oxazolidinone Ring Leading to the Discovery of Anacetrapib

(2011) Cameron J. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanistic Studies of Wacker-Type Intramolecular Aerobic Oxidative Amination of Alkenes Catalyzed by Pd(OAc)2/Pyridine

(2011) Xuan Ye et al.   JOURNAL OF ORGANIC CHEMISTRY

Activated Metallic Gold as an Agent for Direct Methoxycarbonylation

(2011) Bingjun Xu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

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

Iron-Catalyzed Direct Alkenylation of 2-Substituted Azaarenes withN-Sulfonyl Aldimines via C–H Bond Activation

(2011) Bo Qian et al.   ORGANIC LETTERS

Quantification of the Sixth DNA Base Hydroxymethylcytosine in the Brain

(2010) Martin Münzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Potent and highly selective DP1 antagonists with 2,3,4,9-tetrahydro-1H-carbazole as pharmacophore

(2010) Lianhai Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Graphical Journey of Innovative Organic Architectures That Have Improved Our Lives

(2010) Nicholas A. McGrath et al.   JOURNAL OF CHEMICAL EDUCATION

Discovery of a Selective Small-Molecule Melanocortin-4 Receptor Agonist with Efficacy in a Pilot Study of Sexual Dysfunction in Humans

(2010) Mark I. Lansdell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein−Ligand X-ray Structure and Biological Evaluation

(2010) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

DNA Methylation Increases Nucleosome Compaction and Rigidity

(2010) John S. Choy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Quantification of 1,8-cineole and of its metabolites in humans using stable isotope dilution assays

(2010) Kathie Horst et al.   MOLECULAR NUTRITION & FOOD RESEARCH

Catalytic SN2′-Selective Substitution of Allylic Chlorides With Arylboronic Esters

(2010) Aaron M. Whittaker et al.   ORGANIC LETTERS

Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

(2010) Alexander Pasternak et al.   ACS Medicinal Chemistry Letters

Cyclopropenylcarbinol Derivatives as New Versatile Intermediates in Organic Synthesis: Application to the Formation of Enantiomerically Pure Alkylidenecyclopropane Derivatives

(2009) Samah Simaan et al.   CHEMISTRY-A EUROPEAN JOURNAL

Energetics and Reaction Mechanisms for the Competitive Losses of H2, CH4 and C2H4 from Protonated Methylbenzenes—Implications to the Methanol-to-Hydrocarbons (MTH) Process

(2009) Osamu Sekiguchi et al.   EUROPEAN JOURNAL OF MASS SPECTROMETRY

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthetic Studies onN-Alkoxyamines: A Mild and Broadly Applicable Route Starting from Nitroxide Radicals and Aldehydes

(2009) Kai-Uwe Schoening et al.   JOURNAL OF ORGANIC CHEMISTRY

Zn-Mediated, Pd-Catalyzed Cross-Couplings in Water at Room TemperatureWithoutPrior Formation of Organozinc Reagents

(2009) Arkady Krasovskiy et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Degradation of sulfamethoxazole in water by solar photo-Fenton. Chemical and toxicological evaluation

(2009) Alam G. Trovó et al.   WATER RESEARCH

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

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

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

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

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity

(2008) Richard Angell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors

(2008) David J. Kopecky et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Synthesis of 19-trideuteratedent-testosterone and the GABAAreceptor potentiatorsent-androsterone andent-etiocholanolone

(2008) Shirisha Komarapuri et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Novel 4-(4-Aryl)cyclohexyl-1-(2-pyridyl)piperazines as Δ8−Δ7Sterol Isomerase (Emopamil Binding Protein) Selective Ligands with Antiproliferative Activity

(2008) Francesco Berardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of enantiomerically enriched isotopically-labelled anilines by (−)-sparteine directed lithiation

(2008) Jonathan Clayden et al.   TETRAHEDRON-ASYMMETRY