Fluorinated Cycloalkyl Building Blocks for Drug Discovery

Intermolecular Interactions of Organic Fluorine Seen in Perspective

(2022) Jason C. Cole et al.   CRYSTAL GROWTH & DESIGN

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

The preparation and properties of 1,1-difluorocyclopropane derivatives

(2021) Kymbat S Adekenova et al.   Beilstein Journal of Organic Chemistry

Last of the gem‐Difluorocycloalkanes 2: Synthesis of Fluorinated Cycloheptane Building Blocks

(2021) Maksym Herasymchuk et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Fluorinated Rings: Conformation and Application

(2021) Zackaria Nairoukh et al.   CHEMISTRY-A EUROPEAN JOURNAL

Optimized Monofluoromethylsulfonium Reagents for Fluoromethylene-Transfer Chemistry

(2021) Arturs Sperga et al.   JOURNAL OF ORGANIC CHEMISTRY

Photoredox-Catalyzed Addition of Dibromofluoromethane to Alkenes: Direct Synthesis of 1-Bromo-1-fluoroalkanes

(2021) Feng Chen et al.   ORGANIC LETTERS

Nickel-Catalyzed Cross-Electrophile Coupling of the Difluoromethyl Group for Fluorinated Cyclopropane Synthesis

(2021) Elizabeth R. Jarvo et al.   SYNLETT

Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer

(2021) Linrong Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening

(2021) Jeremy S. Disch et al.   JOURNAL OF MEDICINAL CHEMISTRY

gem-Difluorination of Methylenecyclopropanes (MCPs) Featuring a Wagner–Meerwein Rearrangement: Synthesis of 2-Arylsubstituted gem-Difluorocyclobutanes

(2021) Peng-Peng Lin et al.   ORGANIC LETTERS

Photoredox-Mediated Mono- and Difluorination of Remote Unactivated Methylene C(sp3)–H Bonds of N-Alkyl Sulfonamides

(2021) Zhiqiang Deng et al.   ORGANIC LETTERS

Janus all‐cis 2,3,4,5,6‐pentafluorocyclohexyl building blocks applied to medicinal chemistry and bioactives discovery chemistry’

(2021) David O'Hagan et al.   CHEMISTRY-A EUROPEAN JOURNAL

Electrochemically promoted decarboxylative borylation of alkyl N-hydroxyphthalimide esters

(2021) Jian-Jun Dai et al.   CHINESE CHEMICAL LETTERS

Emerging building blocks for medicinal chemistry: recent synthetic advances

(2021) Oleksandr O Grygorenko et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Rational Alteration of Pharmacokinetics of Chiral Fluorinated and Deuterated Derivatives of Emixustat for Retinal Therapy

(2021) Eliav Blum et al.   JOURNAL OF MEDICINAL CHEMISTRY

Large-Scale Cyclopropanation of Butyl Acrylate with Difluorocarbene and Classical Resolution of a Key Fluorinated Building Block

(2021) Adam E. Goetz et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

(2021) Aleša Bricelj et al.   Frontiers in Chemistry

Synthesis and biological evaluation of novel PET tracers [18F]AG120 & [18F]AG135 for imaging mutant isocitrate dehydrogenase 1 expression

(2021) Tingting Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors

(2021) Mitchell H. Keylor et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel, Selective c-Abl Inhibitor, Compound 5, Prevents Neurodegeneration in Parkinson’s Disease

(2021) Seung-Hwan Kwon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Guided Design of Potent Inhibitors of SARS-CoV-2 3CL Protease: Structural, Biochemical, and Cell-Based Studies

(2021) Chamandi S. Dampalla et al.   JOURNAL OF MEDICINAL CHEMISTRY

Iodine-Mediated Fluorination of Alkenes with an HF Reagent: Regioselective Synthesis of 2-Fluoroalkyl Iodides

(2021) Tsugio Kitamura et al.   JOURNAL OF ORGANIC CHEMISTRY

Scalable Synthesis of (R,R)-N,N-Dibenzyl-2-fluorocyclohexan-1-amine with CsF under Hydrogen Bonding Phase-Transfer Catalysis

(2021) Anna Chiara Vicini et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Polar organofluorine substituents: Multivicinal fluorines on alkyl chains and alicyclic rings

(2020) David O'Hagan   CHEMISTRY-A EUROPEAN JOURNAL

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

(2020) Benjamin Jeffries et al.   JOURNAL OF MEDICINAL CHEMISTRY

δ-C–H Mono- and Dihalogenation of Alcohols

(2020) Alastair N. Herron et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Access to Unnatural α-Amino Acids via Visible-Light-Mediated Decarboxylative Conjugate Addition to Dehydroalanine

(2020) Akshay A. Shah et al.   ORGANIC LETTERS

Semi-Industrial Fluorination of β-Keto Esters with SF4: Safety vs Efficacy

(2020) Serhii A. Trofymchuk et al.   SYNLETT

An Iodine‐Catalysis Approach to C(sp3)‐H Fluorination with Nucleophilic Fluorine

(2020) Daniel Bafaluy et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential

(2020) Hiroki Sakai et al.   BIOORGANIC & MEDICINAL CHEMISTRY

gem -Difluorocyclopropanation of Alkenyl Trifluoroborates with the CF3 SiMe3 -NaI System

(2020) Oleksandr V. Hryshchuk et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Pd-Catalyzed γ-C(sp3)–H Fluorination of Free Amines

(2020) Yan-Qiao Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Contribution of Organofluorine Compounds to Pharmaceuticals

(2020) Munenori Inoue et al.   ACS Omega

Fluorine induced pseudo‐anomeric effects in methoxycyclohexanes through electrostatic 1,3‐diaxial interactions

(2020) Bruno A Piscelli et al.   CHEMISTRY-A EUROPEAN JOURNAL

Remote Fluorination and Fluoroalkyl(thiol)ation Reactions

(2020) Ilan Marek et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors

(2020) Guofeng Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Difluorocarbene Generation from TMSCF3: Kinetics and Mechanism of NaI-Mediated and Si-Induced Anionic Chain Reactions

(2020) Andrés García-Domínguez et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Practical and Scalable Synthesis of a Glucokinase Activator via One-Pot Difluorination and Julia Olefination

(2020) Hideyoshi Tsuchiya et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice

(2020) Athri D. Rathnayake et al.   Science Translational Medicine

Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers

(2020) Aymeric Dolbois et al.   ACS Medicinal Chemistry Letters

Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity

(2020) James J. Crawford et al.   ACS Medicinal Chemistry Letters

Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling

(2020) Jeffrey K. Holden et al.   Cell Reports

Molecular Mechanism of Selective Binding of NMS-P118 to PARP-1 and PARP-2: A Computational Perspective

(2020) Ran Wang et al.   Frontiers in Molecular Biosciences

Decarboxylative Borylation of Stabilized and Activated Carbon Radicals

(2020) Qiang Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups

(2020) Benjamin Jeffries et al.   Beilstein Journal of Organic Chemistry

Silver‐Promoted Fluorination Reactions of α‐Bromoamides

(2020) Satoshi Mizuta et al.   CHEMISTRY-A EUROPEAN JOURNAL

Decarboxylative Amination: Diazirines as Single and Double Electrophilic Nitrogen Transfer Reagents

(2020) Preeti P. Chandrachud et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of a Scalable Synthesis of trans-4-Fluorocyclohexylamine via Directed Hydrogenation

(2020) Joyce C. Leung et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Moving targets in drug discovery

(2020) Barbara Zdrazil et al.   Scientific Reports

Discovery of Novel 7-[(1R,5S)-1-Amino-5-fluoro-3-azabicyclo[3.3.0]octan-3-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropane]-8-(methoxy or methyl)quinolones

(2019) Satoshi Komoriya et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based design of inhibitors selective for human proteasome β2c or β2i subunits

(2019) Bo-Tao Xin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors

(2019) Chunjian Liu et al.   ACS Medicinal Chemistry Letters

Hydrogen Bonding Phase-Transfer Catalysis with Potassium Fluoride: Enantioselective Synthesis of β-Fluoroamines

(2019) Gabriele Pupo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery, Optimization, and Biological Characterization of 2,3,6‐Trisubstituted Pyridine‐Containing M 4 Positive Allosteric Modulators

(2019) Jeffrey W. Schubert et al.   ChemMedChem

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

(2019) Miriam Girardini et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Ligand-Promoted Fe(III)-Catalyzed Hydrofluorination of Alkenes

(2019) Mengchun Ye et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Strong hyperconjugative interactions limit solvent and substituent influence on conformational equilibrium: the case of cis-2-halocyclohexylamines

(2019) Camila B Francisco et al.   Beilstein Journal of Organic Chemistry

Fluorine‐Containing Drugs Approved by the FDA in 2018

(2019) Haibo Mei et al.   CHEMISTRY-A EUROPEAN JOURNAL

Last of the gem-Difluorocycloalkanes: Synthesis and Characterization of 2,2-Difluorocyclobutyl-Substituted Building Blocks

(2019) Anton V. Chernykh et al.   JOURNAL OF ORGANIC CHEMISTRY

Review of 18F-Fluciclovine PET for Detection of Recurrent Prostate Cancer

(2019) Mariya Gusman et al.   RADIOGRAPHICS

Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists

(2019) Yufang Xiao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators

(2019) Anthony B. Pinkerton et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stereocontrolled Synthesis of Tetrafluoropentanols: Multivicinal Fluorinated Alkane Units for Drug Discovery

(2019) Patrick Bentler et al.   ORGANIC LETTERS

Diastereoselective Monofluorocyclopropanation Using Fluoromethylsulfonium Salts

(2019) Renate Melngaile et al.   ORGANIC LETTERS

Photoredox-catalyzed deoxyfluorination of activated alcohols with Selectfluor®

(2019) María González-Esguevillas et al.   TETRAHEDRON

Accessing 1,2-Substituted Cyclobutanes through 1,2-Azaborine Photoisomerization

(2019) Zachary X. Giustra et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R)

(2019) María Méndez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Open-Shell Fluorination of Alkyl Bromides: Unexpected Selectivity in a Silyl Radical-Mediated Chain Process

(2019) Gabrielle H. Lovett et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Decarboxylative Borylation of mCPBA-Activated Aliphatic Acids

(2019) Dian Wei et al.   ORGANIC LETTERS

Difluorocarbene as a Building Block for Consecutive Bond-Forming Reactions

(2018) Alexander D. Dilman et al.   ACCOUNTS OF CHEMICAL RESEARCH

Perfluoroalcohols: The Preparation and Crystal Structures of Heptafluorocyclobutanol and Hexafluorocyclobutane-1,1-diol

(2018) Amanda F. Baxter et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small Molecules Targeting Mycobacterium tuberculosis Type II NADH Dehydrogenase Exhibit Antimycobacterial Activity

(2018) Michael B. Harbut et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Amidyl Radicals by Oxidation of α-Amido-oxy Acids: Transition-Metal-Free Amidofluorination of Unactivated Alkenes

(2018) Heng Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fe(II)-Catalyzed Site-selective Functionalization of Unactivated C(sp3)-H Bonds Guided by Alkoxyl Radical

(2018) Lei Liu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fluorinated cyclopropanes: synthesis and chemistry of the aryl α,β,β-trifluorocyclopropane motif

(2018) Connor J. Thomson et al.   CHEMICAL COMMUNICATIONS

The perfluorinated alcohols c-C6F11OH, c-C6F10-1,1-(OH)2 and c-C6F10-1-(CF3)OH

(2018) Jonas Schaab et al.   CHEMICAL COMMUNICATIONS

Synthesis of Functionalized Difluorocyclopropanes: Unique Building Blocks for Drug Discovery

(2018) Roman M. Bychek et al.   CHEMISTRY-A EUROPEAN JOURNAL

Benzylic functionalisation of phenyl all cis-2, 3, 5, 6 -tetrafluoro -cyclohexane provides access to new organo-fluorine building blocks

(2018) David O'Hagan et al.   CHEMISTRY-A EUROPEAN JOURNAL

Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein

(2018) Bhargav A. Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγnull Mouse Model of Malaria

(2018) Aloysius T. Nchinda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Potent Ebola Virus Entry Inhibitors with Suitable Properties for in Vivo Studies

(2018) Hu Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design

(2018) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

The Strength of Hydrogen Bonds between Fluoro-Organics and Alcohols, a Theoretical Study

(2018) Robert E. Rosenberg   JOURNAL OF PHYSICAL CHEMISTRY A

Metal-Free and User-Friendly Regioselective Hydroxyfluorination of Olefins

(2018) Daniel M. Sedgwick et al.   ORGANIC LETTERS

Site-selective 18F fluorination of unactivated C–H bonds mediated by a manganese porphyrin

(2018) Wei Liu et al.   Chemical Science

Metabolism and hydrophilicity of the polarised ‘Janus face’ all-cis tetrafluorocyclohexyl ring, a candidate motif for drug discovery

(2018) Andrea Rodil et al.   Chemical Science

Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET

(2018) Satish K. Chitneni et al.   ACS Medicinal Chemistry Letters

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

(2018) Janeta Popovici-Muller et al.   ACS Medicinal Chemistry Letters

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure–Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization

(2018) Dinakaran Murugesan et al.   ACS Infectious Diseases

Transition Metal-free gem -difluorocyclopropanation of Alkenes with CF3 SiMe3 −NaI System: a Recipe for Electron-deficient Substrates

(2018) Pavel S. Nosik et al.   ADVANCED SYNTHESIS & CATALYSIS

Selective C(sp3)-H and C(sp2)-H Fluorination of Alcohols Using Practical Auxiliaries

(2018) Yang-Jie Mao et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A General Amino Acid Synthesis Enabled by Innate Radical Cross-Coupling

(2018) Phil S. Baran et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Photoinduced Remote Functionalization of Amides and Amines Using Electrophilic Nitrogen Radicals

(2018) Sara P. Morcillo et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Exploring physicochemical space via a bioisostere of the trifluoromethyl and ethyl groups (BITE): attenuating lipophilicity in fluorinated analogues of Gilenya® for multiple sclerosis

(2018) Nathalie Erdeljac et al.   CHEMICAL COMMUNICATIONS

Structure-Based Design of 1-Heteroaryl-1,3-Propanediamine Derivatives as a Novel Series of CC-chemokine Receptor 5 (CCR5) Antagonists

(2018) Panfeng Peng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Novel 7-[(3aS,7aS)-3a-Aminohexahydropyrano[3,4-c]pyrrol-2(3H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens

(2018) Takashi Odagiri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors

(2018) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

The discovery, SAR and biological characterization of a novel series of 6-((1H-pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)

(2018) Sean Bollinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

(2018) Andrew Fensome et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multigram Synthesis of C4/C5 3,3-Difluorocyclobutyl-Substituted Building Blocks

(2018) Sergey Ryabukhin et al.   SYNTHESIS-STUTTGART

Cu-Catalyzed Decarboxylative Borylation

(2018) Jie Wang et al.   ACS Catalysis

Synthesis of 1-hetaryl-2,2-difluorocyclopropane-derived building blocks: The case of pyrazoles

(2018) Pavel S. Nosik et al.   JOURNAL OF FLUORINE CHEMISTRY

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

(2018) Vittoria Zoppi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Diastereoselective α-Fluorination of N-tert-Butanesulfinyl Imidates

(2018) Wei Huang et al.   JOURNAL OF ORGANIC CHEMISTRY

Fluorine multipolar interaction: Toward elucidating its energetics in binding recognition

(2017) Li Xing et al.   JOURNAL OF FLUORINE CHEMISTRY

Partially fluorinated alkoxy groups − Conformational adaptors to changing environments

(2017) Quentin A. Huchet et al.   JOURNAL OF FLUORINE CHEMISTRY

Synthesis of gem -difluorocyclopentane/hexane building blocks

(2017) Kostiantyn P. Melnykov et al.   JOURNAL OF FLUORINE CHEMISTRY

Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

(2017) Pedro Soares et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors

(2017) Carolin Schwehm et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy

(2017) Chih-Chung Tseng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Difluoromethyl Bioisostere: Examining the “Lipophilic Hydrogen Bond Donor” Concept

(2017) Yossi Zafrani et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pd(II)-Catalyzed Enantioselective C(sp3)–H Borylation

(2017) Jian He et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

DrugBank 5.0: a major update to the DrugBank database for 2018

(2017) David S Wishart et al.   NUCLEIC ACIDS RESEARCH

Decarboxylative Borylation of Aliphatic Esters under Visible-Light Photoredox Conditions

(2017) Dawei Hu et al.   ORGANIC LETTERS

Hydrogenation of fluoroarenes: Direct access to all-cis-(multi)fluorinated cycloalkanes

(2017) Mario P. Wiesenfeldt et al.   SCIENCE

Photoinduced decarboxylative borylation of carboxylic acids

(2017) Alexander Fawcett et al.   SCIENCE

Decarboxylative borylation

(2017) Chao Li et al.   SCIENCE

Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling

(2017) R. Moslin et al.   MedChemComm

Site-Selective Tertiary Alkyl-Fluorine Bond Formation from α-Bromoamides Using a Copper/CsF Catalyst System

(2016) Takashi Nishikata et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Photoredox Activation of SF6for Fluorination

(2016) T. Andrew McTeague et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Chemical Probe for the ATAD2 Bromodomain

(2016) Paul Bamborough et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Exploration of bivalent ligands targeting putative mu opioid receptor and chemokine receptor CCR5 dimerization

(2016) Christopher K. Arnatt et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

(2016) Andrew P. Degnan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Achieving regio- and stereo-control in the fluorination of aziridines under acidic conditions

(2016) Otome E. Okoromoba et al.   CHEMICAL COMMUNICATIONS

Polar alicyclic rings: synthesis and structure of all cis-1,2,3,4-tetrafluorocyclopentane

(2016) Zeguo Fang et al.   CHEMICAL COMMUNICATIONS

Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II–III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas

(2016) Yu Zhou et al.   CHEMICAL REVIEWS

Influence of Alcohol β-Fluorination on Hydrogen-Bond Acidity of Conformationally Flexible Substrates

(2016) Jerome Graton et al.   CHEMISTRY-A EUROPEAN JOURNAL

Effect of Partially FluorinatedN-Alkyl-Substituted Piperidine-2-carboxamides on Pharmacologically Relevant Properties

(2016) Raffael Vorberg et al.   ChemMedChem

Janus all-cis-1,2,3,4,5,6-Hexafluorocyclohexane: A Molecular Motif for Aggregation-Induced Enhanced Polarization

(2016) Saied Md Pratik et al.   CHEMPHYSCHEM

Deoxyfluorination of α- N -phthaloyl cycloalkanones with bis(2-methoxyethyl)aminosulfur trifluoride (Deoxo-Fluor)

(2016) Satoe Ishii et al.   JOURNAL OF FLUORINE CHEMISTRY

Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

(2016) Saleem Ahmad et al.   JOURNAL OF MEDICINAL CHEMISTRY

Theoretical Evidence for the Relevance of n(F) → σ*(C–X) (X = H, C, O, S) Stereoelectronic Interactions

(2016) Eusebio Juaristi et al.   JOURNAL OF ORGANIC CHEMISTRY

Catalytic, Diastereoselective 1,2-Difluorination of Alkenes

(2016) Steven M. Banik et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

Fluorinated liquid crystals: evaluation of selectively fluorinated facially polarised cyclohexyl motifs for liquid crystal applications

(2016) Nawaf Al-Maharik et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Fluorination methods in drug discovery

(2016) Damian E. Yerien et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Strain-release amination

(2016) R. Gianatassio et al.   SCIENCE

Successive C–C bond cleavage, fluorination, trifluoromethylthio- and pentafluorophenylthiolation under metal-free conditions to provide compounds with dual fluoro-functionalization

(2016) Ibrayim Saidalimu et al.   Chemical Science

Ligand-Promoted Borylation of C(sp3 )H Bonds with Palladium(II) Catalysts

(2015) Jian He et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease

(2015) François-René Alexandre et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Transition-metal-free visible-light photoredox catalysis at room-temperature for decarboxylative fluorination of aliphatic carboxylic acids by organic dyes

(2015) Xinxin Wu et al.   CHEMICAL COMMUNICATIONS

Site-Selective Approach to β-Fluorination: Photocatalyzed Ring Opening of Cyclopropanols

(2015) Steven Bloom et al.   CHEMISTRY-A EUROPEAN JOURNAL

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors

(2015) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy

(2015) Gianluca Papeo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein–Ligand Complexes

(2015) Jonathan Pollock et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lead Optimization toward Proof-of-Concept Tools for Huntington’s Disease within a 4-(1H-Pyrazol-4-yl)pyrimidine Class of Pan-JNK Inhibitors

(2015) John Wityak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors

(2015) Emmanuel H. Demont et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorination Patterning: A Study of Structural Motifs That Impact Physicochemical Properties of Relevance to Drug Discovery

(2015) Quentin A. Huchet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Decarboxylative Fluorination of Aliphatic Carboxylic Acids via Photoredox Catalysis

(2015) Sandrine Ventre et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Silver-Catalyzed Ring-Opening Strategy for the Synthesis of β- and γ-Fluorinated Ketones

(2015) Huijun Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

All-cis 1,2,3,4,5,6-hexafluorocyclohexane is a facially polarized cyclohexane

(2015) Neil S. Keddie et al.   Nature Chemistry

Fluorine containing amino acids: synthesis and peptide coupling of amino acids containing the all-cis tetrafluorocyclohexyl motif

(2015) Mohammed Salah Ayoup et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Iron- or silver-catalyzed oxidative fluorination of cyclopropanols for the synthesis of β-fluoroketones

(2015) Shichao Ren et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Generation and Ring Opening of Aziridines in Telescoped Continuous Flow Processes

(2015) Nathanael Hsueh et al.   ORGANIC LETTERS

A Highly Regio- and Stereoselective Synthesis of α-Fluorinated Imides via Fluorination of Chiral Enamides

(2015) Yan-Shuang Xu et al.   ORGANIC LETTERS

A Novel and Selective Fluoride Opening of Aziridines by XtalFluor-E. Synthesis of Fluorinated Diamino Acid Derivatives

(2015) Melinda Nonn et al.   ORGANIC LETTERS

Efficient Palladium-Catalyzed C–H Fluorination of C(sp3)–H Bonds: Synthesis of β-Fluorinated Carboxylic Acids

(2015) Qihua Zhu et al.   ORGANIC LETTERS

Iodofluorination of Alkenes Using IF5–Pyridine–HF

(2015) Shoji Hara et al.   SYNTHESIS-STUTTGART

Mild and selective α-fluorination of carbonyl compounds (ketones, 1,3-diketones, β-ketoesters, α-nitroketones, and β-ketonitriles) with Selectfluor (F-TEDA-BF4) in imidazolium ILs [BMIM/PF6 or BMIM/NTf2] with Brønsted-acidic IL [PMIM(SO3H)/OTf] as promoter

(2015) A. Srinivas Reddy et al.   TETRAHEDRON LETTERS

Synthesis, characterization, and nucleophilic ring opening reactions of cyclohexyl-substituted β-haloamines and aziridinium ions

(2015) Hyun-Soon Chong et al.   TETRAHEDRON LETTERS

Development of subnanomolar radiofluorinated (2-pyrrolidin-1-yl)imidazo[1,2-b]pyridazine pan-Trk inhibitors as candidate PET imaging probes

(2015) Vadim Bernard-Gauthier et al.   MedChemComm

Palladium-Catalyzed Iodofluorination of Alkenes Using Fluoro-Iodoxole Reagent

(2015) Nadia O. Ilchenko et al.   ACS Catalysis

A Convenient Photocatalytic Fluorination of Unactivated CH Bonds

(2014) Shira D. Halperin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Simple Sulfinate Synthesis Enables CH Trifluoromethylcyclopropanation

(2014) Ryan Gianatassio et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mechanism of Quinolone Action and Resistance

(2014) Katie J. Aldred et al.   BIOCHEMISTRY

Visible light-promoted metal-free sp3-C–H fluorination

(2014) Ji-Bao Xia et al.   CHEMICAL COMMUNICATIONS

Synthesis and Elaboration of All-cis-1,2,4,5-Tetrafluoro-3-Phenylcyclohexane: A Polar Cyclohexane Motif

(2014) Alastair J. Durie et al.   CHEMISTRY-A EUROPEAN JOURNAL

Fluorine as a Hydrogen-Bond Acceptor: Experimental Evidence and Computational Calculations

(2014) Claudio Dalvit et al.   CHEMISTRY-A EUROPEAN JOURNAL

Simple Vector Considerations to Assess the Polarity of Partially Fluorinated Alkyl and Alkoxy Groups

(2014) Klaus Müller   CHIMIA

Identification and pharmacological characterization of 3,6-diazabicyclo[3.1.1]heptane-3-carboxamides as novel ligands for the α4β2 and α6/α3β2β3 nicotinic acetylcholine receptors (nAChRs)

(2014) Jon-Paul Strachan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Nonbasic Melanin Hormone Receptor 1 Antagonist as an Antiobesity Clinical Candidate

(2014) William N. Washburn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stereoselective Synthesis of cis-2-Fluorocyclopropanecarboxylic Acid

(2014) Taku Shibue et al.   JOURNAL OF ORGANIC CHEMISTRY

Stepwise Preparation of All-cis 1,3,4-Trifluoro-2-phenylcyclohexane, Avoiding a Phenonium Intermediate

(2014) Alastair J. Durie et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis ofgem-Difluorocyclopropa(e)nes and O-, S-, N-, and P-Difluoromethylated Compounds with TMSCF2Br

(2013) Lingchun Li et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells

(2013) Zenyu Shiokawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators

(2013) Mathivanan Packiarajan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fluorine in Pharmaceutical Industry: Fluorine-Containing Drugs Introduced to the Market in the Last Decade (2001–2011)

(2013) Jiang Wang et al.   CHEMICAL REVIEWS

Direct N-gem-difluorocyclopropylation of nitro-heterocycles by utilizing gem-difluorocyclopropyl tosylate

(2013) Wei-Peng Gu et al.   CHINESE CHEMICAL LETTERS

Lead identification of novel and selective TYK2 inhibitors

(2013) Jun Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Co(salen)-mediated enantioselective radiofluorination of epoxides. Radiosynthesis of enantiomerically enriched [18F]F-MISO via kinetic resolution

(2013) Evgeny Revunov et al.   JOURNAL OF FLUORINE CHEMISTRY

On the polarity of partially fluorinated methyl groups

(2013) Quentin A. Huchet et al.   JOURNAL OF FLUORINE CHEMISTRY

Lead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors

(2013) Jun Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2-a]pyrazine Scaffold as a Novel Proline Mimetic

(2013) Kentaro Hashimoto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Silver-Catalyzed Radical Phosphonofluorination of Unactivated Alkenes

(2013) Chengwei Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

1-Amino-4,4-difluorocyclohexanecarboxylic acid as a promising building block for drug discovery: design, synthesis and characterization

(2013) Pavel K. Mykhailiuk et al.   TETRAHEDRON

Enantioselective fluoride ring opening of aziridines enabled by cooperative Lewis acid catalysis

(2013) Julia A. Kalow et al.   TETRAHEDRON

A convenient approach towards the 1-aminomethyl-1-fluorocycloalkane scaffold

(2013) Matthias Moens et al.   TETRAHEDRON LETTERS

Enzymatic preparation of (1S,2R)- and (1R,2S)-stereoisomers of 2-halocycloalkanols

(2013) Olga O. Kolodiazhna et al.   TETRAHEDRON-ASYMMETRY

Discovery of ML314, a Brain Penetrant Nonpeptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor

(2013) Satyamaheshwar Peddibhotla et al.   ACS Medicinal Chemistry Letters

The Synthesis of η-1,2,3,4,5,6-Hexafluorocyclohexane (Benzene Hexafluoride) from Benzene

(2012) Alastair J. Durie et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Investigations into the synthesis, radiofluorination and conjugation of a new [18F]fluorocyclobutyl prosthetic group and its in vitro stability using a tyrosine model system

(2012) Dominic Franck et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators

(2012) Mathivanan Packiarajan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors

(2012) Michael M. Miller et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fluorocyclohexanes: synthesis and structure of all-syn-1,2,4,5-tetrafluorocyclohexane

(2012) Alastair J. Durie et al.   CHEMICAL COMMUNICATIONS

Syntheses and Applications of Monofluorinated Cyclopropanes

(2012) Emilie David et al.   CHEMISTRY-A EUROPEAN JOURNAL

Recent Progress in Small Molecule CCR5 Antagonists as Potential HIV-1 Entry Inhibitors

(2012) Wenwen Chen et al.   CURRENT PHARMACEUTICAL DESIGN

Synthesis and phosphonate binding of guanidine-functionalized fluorinated amphiphiles

(2012) Xinping Wu et al.   JOURNAL OF FLUORINE CHEMISTRY

Halofluorination of alkenes mediated by 1,1,3,3,3-pentafluoropropene-diethylamine adduct

(2012) Justyna Walkowiak et al.   JOURNAL OF FLUORINE CHEMISTRY

Methyl 2,2-Difluoro-2-(fluorosulfonyl)acetate, a Difluorocarbene Reagent with Reactivity Comparable to That of Trimethylsilyl 2,2-Difluoro-2-(fluorosulfonyl)acetate (TFDA)

(2012) Steffen Eusterwiemann et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis of β-Fluoroamines by Lewis Base Catalyzed Hydrofluorination of Aziridines

(2012) Julia A. Kalow et al.   JOURNAL OF ORGANIC CHEMISTRY

Stereocontrolled 1,3-Phosphatyloxy and 1,3-Halogen Migration Relay toward Highly Functionalized 1,3-Dienes

(2012) Roohollah Kazem Shiroodi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Silver-Catalyzed Decarboxylative Fluorination of Aliphatic Carboxylic Acids in Aqueous Solution

(2012) Feng Yin et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Broad-Spectrum Antivirals against 3C or 3C-Like Proteases of Picornaviruses, Noroviruses, and Coronaviruses

(2012) Y. Kim et al.   JOURNAL OF VIROLOGY

Influence of the difluoromethylene group (CF2) on the conformation and properties of selected organic compounds

(2012) David O'Hagan et al.   PURE AND APPLIED CHEMISTRY

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

(2012) W. Liu et al.   SCIENCE

Synthesis of β-Fluoro Amides Using Partially Hydrated Nickel Difluoride as Fluorine Source

(2012) Wan Zhang et al.   SYNLETT

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo

(2012) Janeta Popovici-Muller et al.   ACS Medicinal Chemistry Letters

Synthesis of gem-Difluorinated Cyclopropanes and Cyclopropenes: Trifluoromethyltrimethylsilane as a Difluorocarbene Source

(2011) Fei Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of a Novel Class of Orally Active Antifungal β-1,3-d-Glucan Synthase Inhibitors

(2011) Scott S. Walker et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The synthesis and structure–activity relationship of pyridazinones as glucan synthase inhibitors

(2011) Pauline C. Ting et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of bacterial NAD+-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series

(2011) Suzanne S. Stokes et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and structure of all-syn-1,2,3,4-tetrafluorocyclohexane

(2011) Alastair J. Durie et al.   CHEMICAL COMMUNICATIONS

The fluorine atom as a halogen bond donor, viz. a positive site

(2011) Pierangelo Metrangolo et al.   CRYSTENGCOMM

Learning lessons from drugs that have recently entered the market

(2011) Simon J. Teague   DRUG DISCOVERY TODAY

Pharmacodynamic and pharmacokinetic profile of RBx 343E48F0: A novel, long acting muscarinic receptor antagonist

(2011) Suman Gupta et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Ionic liquids as media for nucleophilic ring opening fluorination of aziridines

(2011) Shun Noritake et al.   HETEROCYCLIC COMMUNICATIONS

Enantioselective Organocatalytic α-Fluorination of Cyclic Ketones

(2011) Piotr Kwiatkowski et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Small molecule inhibitors reveal Niemann–Pick C1 is essential for Ebola virus infection

(2011) Marceline Côté et al.   NATURE

Highly Diastereoselective and General Synthesis of Primary β-Fluoroamines

(2011) Michael L. Schulte et al.   ORGANIC LETTERS

Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc

(2010) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists

(2010) David M. Rotstein et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist

(2010) Xiangyang Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Recently patented and promising ORL-1 ligands: where have we been and where are we going?

(2010) Tally M Largent-Milnes et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Fluorine in health care: Organofluorine containing blockbuster drugs

(2010) David O’Hagan   JOURNAL OF FLUORINE CHEMISTRY

Conformational Analysis ofcis-2-Halocyclohexanols; Solvent Effects by NMR and Theoretical Calculations

(2010) Ernani A. Basso et al.   JOURNAL OF ORGANIC CHEMISTRY

Discovery of 4-tert-Butyl-2,6-dimethylphenylsulfur Trifluoride as a Deoxofluorinating Agent with High Thermal Stability as Well as Unusual Resistance to Aqueous Hydrolysis, and Its Diverse Fluorination Capabilities Including Deoxofluoro-Arylsulfinylation with High Stereoselectivity

(2010) Teruo Umemoto et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Ring Opening of Epoxides by Fluoride Anion Promoted by a Cooperative Dual-Catalyst System

(2010) Julia A. Kalow et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A 1H NMR and theoretical investigation of the conformations of some monosubstituted cyclobutanes

(2010) Raymond J. Abraham et al.   MAGNETIC RESONANCE IN CHEMISTRY

Highly Efficient Diastereoselective Reduction of α-Fluoroimines

(2010) Roy M. Malamakal et al.   ORGANIC LETTERS

Trifluoromethyl-substituted cyclopropanes

(2010) Oleksandr O. Grygorenko et al.   TETRAHEDRON

Maraviroc in the treatment of HIV infection

(2010) Neela Ray   Drug Design Development and Therapy

1-Amido-1-phenyl-3-piperidinylbutanes – CCR5 antagonists for the treatment of HIV: Part 2

(2009) Christopher G. Barber et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists

(2009) Kensuke Kobayashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: Exploration and optimization of alternative pyrazole structure

(2009) Yuichi Sugimoto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of MK-1925: A selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist

(2009) Kensuke Kobayashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles

(2009) Rémy C. Lemoine et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel thioamide derivatives as neutral CB1 receptor antagonists

(2009) Jonas Boström et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel small molecule bradykinin B1 receptor antagonists. Part 3: Hydroxyurea derivatives

(2009) Karsten Schnatbaum et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fluorine Bonding — How Does It Work In Protein−Ligand Interactions?

(2009) Peng Zhou et al.   Journal of Chemical Information and Modeling

Synthesis and Evaluation of a Series of Heterobiarylamides That Are Centrally Penetrant Metabotropic Glutamate Receptor 4 (mGluR4) Positive Allosteric Modulators (PAMs)

(2009) Darren W. Engers et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reaction of difluorocarbene with propargyl esters and efficient synthesis of difluorocyclopropyl ketones

(2009) Xiao-Chun Hang et al.   TETRAHEDRON

Asymmetric syntheses of (1r,3R,4S)- and (1s,3R,4S)-(3,4-difluorocyclopentyl)-alanine derivatives

(2009) Robert D. Simpson et al.   TETRAHEDRON-ASYMMETRY

Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile

(2008) Scott D. Kuduk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors

(2008) Osamu Irie et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)

(2008) Kevin J. Moriarty et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Orally Bioavailable Cathepsin S Inhibitors for the Reversal of Neuropathic Pain

(2008) Osamu Irie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Influence of relative configuration of disubstituted cyclopentanes and -hexanes on13C shifts

(2008) Margit Winkler et al.   MAGNETIC RESONANCE IN CHEMISTRY

Development of a Bulk Enabling Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist

(2008) Sarah J. Haycock-Lewandowski et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

A general route for the synthesis of β,β-difluorocarboxylic acids

(2008) Or Cohen et al.   TETRAHEDRON

α-Hydroxy amides as a novel class of bradykinin B1 selective antagonists

(2007) Michael R. Wood et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS