Fluorination methods in drug discovery

Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity

(2016) Jizhen Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Catalytic C–F bond activation of geminal difluorocyclopropanes by nickel(i) complexes via a radical mechanism

(2016) Jan Wenz 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

18F-Labeling of Arenes and Heteroarenes for Applications in Positron Emission Tomography

(2016) Sean Preshlock et al.   CHEMICAL REVIEWS

[18F]-Group 13 fluoride derivatives as radiotracers for positron emission tomography

(2016) Kantapat Chansaenpak et al.   CHEMICAL SOCIETY REVIEWS

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

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

Mono- and Difluorination of Benz­ylic Carbon Atoms

(2016) Ana Koperniku et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Methyl NFSI: atom-economical alternative to NFSI shows higher fluorination reactivity under Lewis acid-catalysis and non-catalysis

(2016) Kazunobu Fukushi et al.   GREEN CHEMISTRY

Sustainable synthesis of enantiopure fluorolactam derivatives by a selective direct fluorination – amidase strategy

(2016) Nicky J. Willis et al.   GREEN CHEMISTRY

Regioselective Electrophilic Fluorination of Rationally Designed Imidazole Derivatives

(2016) Klaus Albertshofer et al.   JOURNAL OF ORGANIC CHEMISTRY

Enantioselective aldol reactions with masked fluoroacetates

(2016) Jakub Saadi et al.   Nature Chemistry

The total synthesis of calcium atorvastatin

(2016) Luiz C. Dias et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Pd(II)-Catalyzed Aminofluorination of Alkenes in Total Synthesis 6-(R)-Fluoroswainsonine and 5-(R)-Fluorofebrifugine

(2016) Liang Wu et al.   ORGANIC LETTERS

Diastereoselective Synthesis and Conformational Analysis of (2R)- and (2S)-Fluorostatines: An Approach Based on Organocatalytic Fluorination of a Chiral Aldehyde

(2016) Xiang-Guo Hu et al.   ORGANIC LETTERS

Aminofluorination: transition-metal-free N–F bond insertion into diazocarbonyl compounds

(2016) Gui Chen et al.   Chemical Science

Asymmetric 18F-fluorination for applications in positron emission tomography

(2016) Faye Buckingham et al.   Chemical Science

Organomediated Enantioselective18F Fluorination for PET Applications

(2015) Faye Buckingham et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

18F-Labeling of Aryl-SCF3, -OCF3and -OCHF2with [18F]Fluoride

(2015) Tanatorn Khotavivattana et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Triazole: A Promising Antitubercular Agent

(2015) Rangappa S. Keri et al.   Chemical Biology & Drug Design

Direct photocatalytic fluorination of benzylic C–H bonds with N-fluorobenzenesulfonimide

(2015) Matthew B. Nodwell et al.   CHEMICAL COMMUNICATIONS

Photochemical Fluorination Reactions - A Promising Research Field for Continuous-Flow Synthesis

(2015) Thomas H. Rehm   CHEMICAL ENGINEERING & TECHNOLOGY

Introduction: Fluorine Chemistry

(2015) Veronique Gouverneur et al.   CHEMICAL REVIEWS

Monofluorination of Organic Compounds: 10 Years of Innovation

(2015) Pier Alexandre Champagne et al.   CHEMICAL REVIEWS

A Fluorination/Aryl Migration/Cyclization Cascade for the Metal-Free Synthesis of Fluoro-Benzoxazepines

(2015) Anna Ulmer et al.   CHEMISTRY-A EUROPEAN JOURNAL

Organocatalytic Asymmetric Fluorination of 4-Substituted Isoxazolinones

(2015) Huanrui Zhang et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Small-Molecule Therapeutics for Ebola Virus (EBOV) Disease Treatment

(2015) Kunisuke Izawa et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Advancements in Aminofluorination of Alkenes and Alkynes: Convenient Access to β-Fluoroamines

(2015) Pinhong Chen et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Synthesis of 5-Fluorotriazoles by Silver-Mediated Fluorination of 5-Iodotriazoles

(2015) Damin Wang et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Organofluorine chemistry: applications, sources and sustainability

(2015) Antal Harsanyi et al.   GREEN CHEMISTRY

Synthesis of fluorinated oxygen- and sulfur-containing heteroaromatics

(2015) Eileen M. O’Leary et al.   JOURNAL OF FLUORINE CHEMISTRY

Oxidative fluorination of N-arylsulfonamides

(2015) Faye Buckingham et al.   JOURNAL OF FLUORINE 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

Investigation and Conformational Analysis of Fluorinated Nucleoside Antibiotics Targeting Siderophore Biosynthesis

(2015) Surendra Dawadi et al.   JOURNAL OF ORGANIC CHEMISTRY

Transition-Metal-Free Oxyfluorination of Olefinic Amides for the Synthesis of Fluorinated Heterocycles

(2015) Jing-Feng Zhao et al.   JOURNAL OF ORGANIC CHEMISTRY

Anhydrous Tetramethylammonium Fluoride for Room-Temperature SNAr Fluorination

(2015) Sydonie D. Schimler et al.   JOURNAL OF ORGANIC CHEMISTRY

Regioselective Fluorination of Imidazo[1,2-a]pyridines with Selectfluor in Aqueous Condition

(2015) Ping Liu et al.   JOURNAL OF ORGANIC CHEMISTRY

A Fluorinated Ligand Enables Room-Temperature and Regioselective Pd-Catalyzed Fluorination of Aryl Triflates and Bromides

(2015) Aaron C. Sather et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

PyFluor: A Low-Cost, Stable, and Selective Deoxyfluorination Reagent

(2015) Matthew K. Nielsen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Fluorination of 2-substituted benzo[b]furans with Selectfluor™

(2015) Mingliang Wang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

(2015) Qihua Zhu et al.   ORGANIC LETTERS

Development of a Direct Photocatalytic C–H Fluorination for the Preparative Synthesis of Odanacatib

(2015) Shira D. Halperin et al.   ORGANIC LETTERS

Asymmetric Fluorination Approach to the Scalable Synthesis of a SYK Inhibitor

(2015) Neil R. Curtis et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Selective C–H Bond Fluorination of Phenols with a Removable Directing Group: Late-Stage Fluorination of 2-Phenoxyl Nicotinate Derivatives

(2015) Shao-Jie Lou et al.   ACS Catalysis

Transition-metal free oxidative aliphatic C–H fluorination

(2015) Xiaofei Zhang et al.   Organic Chemistry Frontiers

Asymmetric Fluorocyclizations of Alkenes

(2014) Jamie R. Wolstenhulme et al.   ACCOUNTS OF CHEMICAL RESEARCH

Inside Cover: Thiophene-Based, Radial π-Conjugation: Synthesis, Structure, and Photophysical Properties of Cyclo-1,4-phenylene-2′,5′-thienylenes (Angew. Chem. Int. Ed. 1/2015)

(2014) Hideto Ito et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A General Copper-Mediated Nucleophilic18F Fluorination of Arenes

(2014) Matthew Tredwell et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The synthesis of gemcitabine

(2014) Kylie Brown et al.   CARBOHYDRATE RESEARCH

Silver-catalyzed one-pot cyclization/fluorination of 2-alkynylanilines: highly efficient synthesis of structurally diverse fluorinated indole derivatives

(2014) Lei Yang et al.   CHEMICAL COMMUNICATIONS

Modern Carbon–Fluorine Bond Forming Reactions for Aryl Fluoride Synthesis

(2014) Michael G. Campbell et al.   CHEMICAL REVIEWS

Advances in Catalytic Enantioselective Fluorination, Mono-, Di-, and Trifluoromethylation, and Trifluoromethylthiolation Reactions

(2014) Xiaoyu Yang et al.   CHEMICAL REVIEWS

Divergent Reaction Mechanisms in the Aminofluorination of Alkenes

(2014) Wangqing Kong et al.   CHIMIA

Palladium-Catalyzed Oxidative Olefination of Phenols Bearing Removable Directing Groups under Molecular Oxygen

(2014) Bin Liu et al.   JOURNAL OF ORGANIC CHEMISTRY

Direct C–F Bond Formation Using Photoredox Catalysis

(2014) Montserrat Rueda-Becerril et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

How Cinchona Alkaloid-Derived Primary Amines Control Asymmetric Electrophilic Fluorination of Cyclic Ketones

(2014) Yu-hong Lam et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A General and Enantioselective Approach to Pentoses: A Rapid Synthesis of PSI-6130, the Nucleoside Core of Sofosbuvir

(2014) Manuel Peifer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Metal-Free, Efficient Oxyfluorination of Olefins for the Synthesis of α-Fluoroketones

(2014) Qiang Yang et al.   ORGANIC LETTERS

Late-Stage Fluorination: From Fundamentals to Application

(2014) Michael G. Campbell et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

PhenoFluor: Practical Synthesis, New Formulation, and Deoxyfluorination of Heteroaromatics

(2014) Teppei Fujimoto et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

On the role of fluoro-substituted nucleosides in DNA radiosensitization for tumor radiation therapy

(2014) J. Kopyra et al.   RSC Advances

Palladium-Catalyzed Decarboxylative Coupling of α- Oxocarboxylic Acids with C(sp2)H of 2-Aryloxypyridines

(2013) Jinzhong Yao et al.   ADVANCED SYNTHESIS & CATALYSIS

Stereoselectively fluorinatedN-heterocycles: a brief survey

(2013) Xiang-Guo Hu et al.   Beilstein Journal of Organic Chemistry

Electrophilic fluorination using a hypervalent iodine reagent derived from fluoride

(2013) Gemma C. Geary et al.   CHEMICAL COMMUNICATIONS

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

(2013) Jiang Wang et al.   CHEMICAL REVIEWS

Ruthenium(II)-Catalyzed CH Alkenylations of Phenols with Removable Directing Groups

(2013) Wenbo Ma et al.   CHEMISTRY-A EUROPEAN JOURNAL

A Two-Step Sequence to Ethyl α-Fluorocyclopropanecarboxylates Through MIRC Reaction of Ethyl Dichloroacetate and Highly Regioselective Fluorination

(2013) Min Zhang et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12receptor

(2013) Peter Bach et al.   Future Medicinal Chemistry

Non-Nucleoside Inhibitors of BasE, an Adenylating Enzyme in the Siderophore Biosynthetic Pathway of the Opportunistic Pathogen Acinetobacter baumannii

(2013) João Neres et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enantioselective Synthesis of cis-3-Fluoropiperidin-4-ol, a Building Block for Medicinal Chemistry

(2013) Simon J. Shaw et al.   JOURNAL OF ORGANIC CHEMISTRY

Late-Stage Deoxyfluorination of Alcohols with PhenoFluor

(2013) Filippo Sladojevich et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mild Copper-Mediated Fluorination of Aryl Stannanes and Aryl Trifluoroborates

(2013) Yingda Ye et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Silver-Catalyzed Radical Phosphonofluorination of Unactivated Alkenes

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

Copper-Mediated Fluorination of Arylboronate Esters. Identification of a Copper(III) Fluoride Complex

(2013) Patrick S. Fier et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Oxidative aliphatic C-H fluorination with manganese catalysts and fluoride ion

(2013) Wei Liu et al.   Nature Protocols

Double Annulative Cascade of Tryptophan-Containing Peptides Triggered by Selectfluor

(2013) Bret Tréguier et al.   ORGANIC LETTERS

One-Pot Gold-Catalyzed Aminofluorination of Unprotected 2-Alkynylanilines

(2013) Antonio Arcadi et al.   ORGANIC LETTERS

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

(2013) P. S. Fier et al.   SCIENCE

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability

(2013) Erik J. Hicken et al.   ACS Medicinal Chemistry Letters

Cover Picture: Champagne and Fireworks:Angewandte ChemieCelebrates Its Birthday (Angew. Chem. Int. Ed. 1/2013)

(2012) Peter Gölitz   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2′,3′-dideoxy-2′,2′-difluoro-4′-azanucleosides

(2012) Saúl Martínez-Montero et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel flavonols as potential anti-prostate cancer agents

(2012) Robert G. Britton et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Zolpidem for insomnia

(2012) David J Greenblatt et al.   EXPERT OPINION ON PHARMACOTHERAPY

Synthesis and applications of fluorinated nucleoside analogues

(2012) Hanna Wójtowicz-Rajchel   JOURNAL OF FLUORINE CHEMISTRY

Fluorine Transfer to Alkyl Radicals

(2012) Montserrat Rueda-Becerril et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Fe(III)/NaBH4-Mediated Free Radical Hydrofluorination of Unactivated Alkenes

(2012) Timothy J. Barker et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Copper-Mediated Fluorination of Aryl Iodides

(2012) Patrick S. Fier 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

Ag(I)-Catalyzed Aminofluorination of Alkynes: Efficient Synthesis of 4-Fluoroisoquinolines and 4-Fluoropyrrolo[α]isoquinolines

(2012) Tao Xu et al.   ORGANIC LETTERS

Metal-Free Ortho C–H Borylation of 2-Phenoxypyridines under Mild Conditions

(2012) Liting Niu et al.   ORGANIC LETTERS

Ruthenium-Catalyzed C–H Bond Arylations of Arenes Bearing Removable Directing Groups via Six-Membered Ruthenacycles

(2012) Lutz Ackermann et al.   ORGANIC LETTERS

Development of Two Complementary Syntheses for a Privileged CGRP Receptor Antagonist Substructure

(2012) David K. Leahy et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

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

(2012) W. Liu et al.   SCIENCE

Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer's disease

(2012) Neil Vasdev et al.   MedChemComm

Ir-catalysed formation of C−F bonds. From allylic alcohols to α-fluoroketones

(2011) Nanna Ahlsten et al.   CHEMICAL COMMUNICATIONS

Transition metal catalysis and nucleophilic fluorination

(2011) Charlotte Hollingworth et al.   CHEMICAL COMMUNICATIONS

Iminosugars as therapeutic agents: recent advances and promising trends

(2011) Robert J Nash et al.   Future Medicinal Chemistry

Pseudomonas stutzeri lipase: a useful biocatalyst for aminolysis reactions

(2011) S. van Pelt et al.   GREEN CHEMISTRY

Deoxyfluorination of Phenols

(2011) Pingping Tang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Organocatalytic α-Fluorination of Cyclic Ketones

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

Catalysis for fluorination and trifluoromethylation

(2011) Takeru Furuya et al.   NATURE

An Efficient Difluorohydroxylation of Indoles Using Selectfluor as a Fluorinating Reagent

(2011) Riyuan Lin et al.   ORGANIC LETTERS

A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging

(2011) E. Lee et al.   SCIENCE

Silver-mediated fluorination of aryl silanes

(2011) Pingping Tang et al.   TETRAHEDRON

Convenient Electrophilic Fluorination of Functionalized Aryl and Heteroaryl Magnesium Reagents

(2010) Shigeyuki Yamada et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fluorine-Enabled Cationic Gold Catalysis: Functionalized Hydration of Alkynes

(2010) Weibo Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Amplification of the Inhibitory Activity and Reversal of the Selectivity of Miglitol by C(2′)-Monofluorination

(2010) Erik Prell et al.   ARCHIV DER PHARMAZIE

Fluorine in health care: Organofluorine containing blockbuster drugs

(2010) David O’Hagan   JOURNAL OF FLUORINE CHEMISTRY

Aminodifluorosulfinium Salts: Selective Fluorination Reagents with Enhanced Thermal Stability and Ease of Handling†,‡

(2010) Alexandre L’Heureux et al.   JOURNAL OF ORGANIC CHEMISTRY

Silver-Catalyzed Late-Stage Fluorination

(2010) Pingping Tang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The flow synthesis of heterocycles for natural product and medicinal chemistry applications

(2010) Marcus Baumann et al.   MOLECULAR DIVERSITY

New Synthesis of Fluorinated Pyrazoles

(2010) Riccardo Surmont et al.   ORGANIC LETTERS

Palladium(II)-CatalyzedOrthoArylation of 2-Phenoxypyridines with Potassium Aryltrifluoroborates via C−H Functionalization

(2010) Jean-Ho Chu et al.   ORGANOMETALLICS

The Organometallic Fluorine Chemistry of Palladium and Rhodium: Studies toward Aromatic Fluorination

(2009) Vladimir V. Grushin   ACCOUNTS OF CHEMICAL RESEARCH

Fluorine in medicinal chemistry: a century of progress and a 60-year retrospective of selected highlights

(2009) Robert Filler et al.   Future Medicinal Chemistry

Semisynthesis, Biological Activity, and Molecular Modeling Studies of C-Ring-Modified Camptothecins†

(2009) Cristian Samorì et al.   JOURNAL OF MEDICINAL CHEMISTRY

Silver-Mediated Fluorination of Functionalized Aryl Stannanes

(2009) Takeru Furuya et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

(2009) Shih-Min A. Huang et al.   NATURE

Palladium-Catalyzed Acylation of sp2C−H bond: Direct Access to Ketones from Aldehydes

(2009) Xiaofei Jia et al.   ORGANIC LETTERS

Fluorination of Boronic Acids Mediated by Silver(I) Triflate

(2009) Takeru Furuya et al.   ORGANIC LETTERS

Formation of ArF from LPdAr(F): Catalytic Conversion of Aryl Triflates to Aryl Fluorides

(2009) D. A. Watson et al.   SCIENCE

Nitrogen-Containing Organofluorine Derivatives: An Overview

(2009) Santos Fustero et al.   SYNLETT

Micellar-System-Mediated Direct Fluorination of Ketones in Water

(2009) Stojan Stavber et al.   SYNLETT

Microwave-assisted aliphatic fluorine–chlorine exchange using triethylamine trihydrofluoride (TREAT-HF)

(2009) Jennifer M. Kremsner et al.   TETRAHEDRON LETTERS

Palladium-Mediated Fluorination of Arylboronic Acids

(2008) Takeru Furuya et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The Many Roles for Fluorine in Medicinal Chemistry

(2008) William K. Hagmann   JOURNAL OF MEDICINAL CHEMISTRY

Highly Regioselective Fluorination and Iodination of Alkynyl Enolates

(2008) Han Yang et al.   ORGANIC LETTERS

Fluorination in Medicinal Chemistry: Methods, Strategies, and Recent Developments

(2008) Kenneth L. Kirk   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Fluorine in medicinal chemistry

(2007) Sophie Purser et al.   CHEMICAL SOCIETY REVIEWS