标题
Fluorinated Cycloalkyl Building Blocks for Drug Discovery
作者
关键词
-
出版物
ChemMedChem
Volume -, Issue -, Pages -
出版商
Wiley
发表日期
2022-08-29
DOI
10.1002/cmdc.202200365
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- Transition-metal-free visible-light photoredox catalysis at room-temperature for decarboxylative fluorination of aliphatic carboxylic acids by organic dyes
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- Site-Selective Approach to β-Fluorination: Photocatalyzed Ring Opening of Cyclopropanols
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- Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors
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- 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
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- Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
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- Applications of Fluorine in Medicinal Chemistry
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- Decarboxylative Fluorination of Aliphatic Carboxylic Acids via Photoredox Catalysis
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- Silver-Catalyzed Ring-Opening Strategy for the Synthesis of β- and γ-Fluorinated Ketones
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- All-cis 1,2,3,4,5,6-hexafluorocyclohexane is a facially polarized cyclohexane
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- Fluorine containing amino acids: synthesis and peptide coupling of amino acids containing the all-cis tetrafluorocyclohexyl motif
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- 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
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- Efficient Palladium-Catalyzed C–H Fluorination of C(sp3)–H Bonds: Synthesis of β-Fluorinated Carboxylic Acids
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- 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
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- Palladium-Catalyzed Iodofluorination of Alkenes Using Fluoro-Iodoxole Reagent
- (2015) Nadia O. Ilchenko et al. ACS Catalysis
- A Convenient Photocatalytic Fluorination of Unactivated CH Bonds
- (2014) Shira D. Halperin et al. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Simple Sulfinate Synthesis Enables CH 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
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- 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
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- 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
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- Silver-Catalyzed Radical Phosphonofluorination of Unactivated Alkenes
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- 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
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- Methyl 2,2-Difluoro-2-(fluorosulfonyl)acetate, a Difluorocarbene Reagent with Reactivity Comparable to That of Trimethylsilyl 2,2-Difluoro-2-(fluorosulfonyl)acetate (TFDA)
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- 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
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- 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
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- Learning lessons from drugs that have recently entered the market
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- Pharmacodynamic and pharmacokinetic profile of RBx 343E48F0: A novel, long acting muscarinic receptor antagonist
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- Ionic liquids as media for nucleophilic ring opening fluorination of aziridines
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- 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
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- 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
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- Enantioselective Ring Opening of Epoxides by Fluoride Anion Promoted by a Cooperative Dual-Catalyst System
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- 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
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