Nucleophilic Halogenation of Heterocyclic N ‐Oxides: Recent Progress and a Practical Guide

Enantioselective Ammonium Ylide Mediated One‐Pot Synthesis of Highly Substituted γ ‐Butyrolactones

(2020) Till Drennhaus et al.   ADVANCED SYNTHESIS & CATALYSIS

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications

(2020) Nagaraju Kerru et al.   MOLECULES

Catalytic enantioselective synthesis of heterocyclic vicinal fluoroamines using asymmetric protonation: A method development and mechanistic study

(2020) Allan J. B. Watson et al.   CHEMISTRY-A EUROPEAN JOURNAL

Co(III)-Catalyzed C–H Amidation of Nitrogen-Containing Heterocycles with Dioxazolones under Mild Conditions

(2020) Ankit Kumar Dhiman et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis of 4-((1H-benzo[d]imidazol-2-yl)oxy)-3-methylpicolinic acid, a key related substance of Rabeprazole sodium

(2020) Xiaoyan He et al.   TETRAHEDRON LETTERS

Synthesis of electrophilic N-heterocyclic carbenes based on azahelicene

(2020) Pierpaolo Morgante et al.   TETRAHEDRON LETTERS

Recent Advances in the Synthesis of C2‐Functionalized Pyridines and Quinolines Using N‐Oxide Chemistry

(2020) Dong Wang et al.   ADVANCED SYNTHESIS & CATALYSIS

Metal-Free Functionalization of Azine N-Oxides with Electrophilic Reagents

(2020) Sergey V. Baykov et al.   Chemistry of Heterocyclic Compounds

Rh/O2-Catalyzed C8 Olefination of Quinoline N-Oxides with Activated and Unactivated Olefins

(2019) Ritika Sharma et al.   JOURNAL OF ORGANIC CHEMISTRY

Tandem Deoxygenation/Halogenation of N -Oxides Under Acylation Conditions: Scope and In Situ IR Spectroscopic Study

(2019) Roman S. Malykhin et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Copper-Catalyzed Regioselective C–H Amination of Phenol Derivatives with Assistance of Phenanthroline-Based Bidentate Auxiliary

(2019) Kazutaka Takamatsu et al.   ACS Catalysis

Substrate-Directed Lewis-Acid Catalysis for Peptide Synthesis

(2019) Wataru Muramatsu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Stereoselective Synthesis of Atropisomeric Bipyridine N,N′-Dioxides by Oxidative Coupling

(2019) Yasuaki Fukazawa et al.   ORGANIC LETTERS

Rh(III)-catalyzed C8 arylation of quinoline N-oxides with arylboronic acids

(2019) Yuanqiong Huang et al.   CHINESE CHEMICAL LETTERS

Nucleophilic Halogenation of Cyclic Nitronates: A General Access to 3-Halo-1,2-Oxazines

(2019) Roman S. Malykhin et al.   JOURNAL OF ORGANIC CHEMISTRY

Pd-Catalyzed Sequential Arylation of 7-Azaindoles: Aggregate-Induced Emission of Tetra-Aryl 7-Azaindoles

(2019) Savio Cardoza et al.   JOURNAL OF ORGANIC CHEMISTRY

Structure-based design and profiling of novel 17β-HSD14 inhibitors

(2018) Florian Braun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Chelation-assisted de-aryloxylative amination of 2-aryloxy quinolines: a new synthetic route to a key fragment of a bioactive PRMT5 inhibitor

(2018) Aniket Gupta et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Heterobicyclic Core Retained Hydroarylations through C–H Activation: Synthesis of Epibatidine Analogues

(2018) Deng-Yuan Li et al.   ORGANIC LETTERS

Bifunctional metal-free photo-organocatalysts for enantioselective aerobic oxidation of β-dicarbonyl compounds

(2018) Xiao-fei Tang et al.   TETRAHEDRON

Design and synthesis of potent RSK inhibitors

(2018) Rama Jain et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The m-CPBA–NH3(g) System: A Safe and Scalable Alternative for the Manufacture of (Substituted) Pyridine and Quinoline N-Oxides

(2018) Amey Palav et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Potent Antimalarial 2-Pyrazolyl Quinolone bc1 (Qi) Inhibitors with Improved Drug-like Properties

(2018) W. David Hong et al.   ACS Medicinal Chemistry Letters

Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1)

(2017) Douglas S. Williamson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Palladium-Catalyzed Directed Halogenation of Bipyridine N-Oxides

(2017) Sina P. Zucker et al.   JOURNAL OF ORGANIC CHEMISTRY

Preparation of the HIV Attachment Inhibitor BMS-663068. Part 5. Selective C-7 Bromination of the 6-Azaindole Core

(2017) Francisco González-Bobes et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

An expeditious synthetic protocol for chlorination of imidazole N -oxide: Synthesis of 2-chloroimidazoles

(2017) Mossaraf Hossain et al.   TETRAHEDRON LETTERS

Adding a Hydrogen Bond May Not Help: Naphthyridinone vs Quinoline Inhibitors of Macrophage Migration Inhibitory Factor

(2017) Thomas K. Dawson et al.   ACS Medicinal Chemistry Letters

Asymmetric α-Hydroxylation of β-Indanone Esters and β-Indanone Amides Catalyzed by C-2′ Substituted Cinchona Alkaloid Derivatives

(2016) Yakun Wang et al.   ADVANCED SYNTHESIS & CATALYSIS

Synthesis and biological evaluation of C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors

(2016) Ho Shin Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Regioselective Chlorination of QuinolineN-Oxides and IsoquinolineN-Oxides Using PPh3/Cl3CCN

(2016) Kai Qiao et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Application of 1,1-ADEQUATE, HMBC, and Density Functional Theory To Determine Regioselectivity in the Halogenation of Pyridine N-Oxides

(2016) Tsang-Lin Hwang et al.   ORGANIC LETTERS

A highly practical and convenient halogenation of fused heterocyclic N -oxides

(2016) Dong Wang et al.   TETRAHEDRON

General methods for the synthesis and late-stage diversification of 2,4-substituted 7-azaindoles

(2016) Jeffrey G. Varnes et al.   TETRAHEDRON LETTERS

Experimental and mechanistic analysis of the palladium-catalyzed oxidative C8-selective C–H homocoupling of quinoline N-oxides

(2015) David E. Stephens et al.   CHEMICAL COMMUNICATIONS

Nucleophilic halogenation of imidazole N-oxides

(2015) Evgeny I. Adiulin et al.   Chemistry of Heterocyclic Compounds

Synthesis of 4-Arylthieno[2,3-b]pyridines and 4-Aminothieno[2,3-b]pyridines via a Regioselective Bromination of Thieno[2,3-b]pyridine

(2015) Simon C. C. Lucas et al.   JOURNAL OF ORGANIC CHEMISTRY

Design, Synthesis, and Protein Crystallography of Biaryltriazoles as Potent Tautomerase Inhibitors of Macrophage Migration Inhibitory Factor

(2015) Pawel Dziedzic et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design of a New Bimetallic Catalyst for Asymmetric Epoxidation and Sulfoxidation

(2015) Sukalyan Bhadra et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Highly Regioselective Halogenation of Pyridine N-Oxide: Practical Access to 2-Halo-Substituted Pyridines

(2015) Ying Chen et al.   ORGANIC LETTERS

Facile Route to 2-Fluoropyridines via 2-Pyridyltrialkylammonium Salts Prepared from Pyridine N-Oxides and Application to 18F-Labeling

(2015) Hui Xiong et al.   ORGANIC LETTERS

Discovery of 4-anilino α-carbolines as novel Brk inhibitors

(2014) Kazem Ahmed Mahmoud et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Modern Carbon–Fluorine Bond Forming Reactions for Aryl Fluoride Synthesis

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

The Discovery of N-((2H-Tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): A Potent and Selective Glucagon Receptor Antagonist

(2014) Duane DeMong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of the 6-Azaindole Containing HIV-1 Attachment Inhibitor Pro-Drug, BMS-663068

(2014) Ke Chen et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis, molecular docking study, and evaluation of the antiproliferative action of a new group of propargylthio- and propargylselenoquinolines

(2014) Krzysztof Marciniec et al.   MEDICINAL CHEMISTRY RESEARCH

Regioselective synthesis of multiply halogenated azaxanthones

(2014) Wenyuan Qian et al.   TETRAHEDRON LETTERS

A practical and mild chlorination of fused heterocyclic N-oxides

(2014) Dong Wang et al.   TETRAHEDRON LETTERS

Novel inhibitors of breast cancer relevant kinases Brk and HER2

(2014) Kazem Ahmed Mahmoud et al.   MedChemComm

Synthetic Studies on Pseudo-Dimeric Lycopodium Alkaloids: Total Synthesis of Complanadine B

(2013) James N. Newton et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

7-Phenyl-imidazoquinolin-4(5H)-one derivatives as selective and orally available mPGES-1 inhibitors

(2013) Tomoya Shiro et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of 4,5-Bis(Dimethylamino)Quinolines and the Dual Direction of their Protonation

(2013) E. A. Shmoilova et al.   Chemistry of Heterocyclic Compounds

Strategies To Reduce hERG K+ Channel Blockade. Exploring Heteroaromaticity and Rigidity in Novel Pyridine Analogues of Dofetilide

(2013) João F. S. Carvalho et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Method for the Preparation of 4-Arylimidazolones

(2013) Duane E. DeMong et al.   ORGANIC LETTERS

Regioselective Bromination of Fused Heterocyclic N-Oxides

(2013) Sarah E. Wengryniuk et al.   ORGANIC LETTERS

Conformationally Rigid Chiral Pyridine N-Oxides as Organocatalyst: Asymmetric Allylation of Aldehydes

(2012) Elumalai Gnanamani et al.   ADVANCED SYNTHESIS & CATALYSIS

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

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

(2012) John Liddle et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis of Pyridine and Dihydropyridine Derivatives by Regio- and Stereoselective Addition to N-Activated Pyridines

(2012) James A. Bull et al.   CHEMICAL REVIEWS

Effects of the Pyridine 3-Substituent on Regioselectivity in the Nucleophilic Aromatic Substitution Reaction of 3-Substituted 2,6-Dichloropyridines with 1-Methylpiperazine Studied by a Chemical Design Strategy

(2012) Peter Bach et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

First Total Syntheses of 1,3-Disubstituted β-Carboline Alkaloids, Dichotomide I and Marinacarbolines A-D

(2012) Satoshi Hibino et al.   HETEROCYCLES

Lead Optimization of 3-Carboxyl-4(1H)-Quinolones to Deliver Orally Bioavailable Antimalarials

(2012) Yiqun Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Asymmetric Synthesis of Trifluoromethylated Amines via Catalytic Enantioselective Isomerization of Imines

(2012) Yongwei Wu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E2 synthase-1 inhibitors

(2011) Tomoya Shiro et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chemistry of Six-Membered Cyclic Oxime Ethers. Application in the Synthesis of Bioactive Compounds

(2011) Alexey Yu. Sukhorukov et al.   CHEMICAL REVIEWS

8-Azatetracyclines: Synthesis and Evaluation of a Novel Class of Tetracycline Antibacterial Agents

(2011) Roger B. Clark et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and structure–activity relationships of antimalarial 4-oxo-3-carboxyl quinolones

(2010) Yiqun Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Microwave-assisted synthesis of quinoline, isoquinoline, quinoxaline and quinazoline derivatives as CB2 receptor agonists

(2010) Raimo Saari et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and modulation properties of imidazo[4,5-b]pyridin-7-one and indazole-4,7-dione derivatives towards the Cryptosporidium parvum CpABC3 transporter

(2010) Waël Zeinyeh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of GSK1070916, a Potent and Selective Inhibitor of Aurora B/C Kinase

(2010) Nicholas D. Adams et al.   JOURNAL OF MEDICINAL CHEMISTRY

Improved Synthesis of the Selective Rho-Kinase Inhibitor 6-Chloro-N4-{3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl}pyrimidin-2,4-diamine

(2010) Hartmut Schirok et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Benzothiophene inhibitors of MK2. Part 2: Improvements in kinase selectivity and cell potency

(2009) David R. Anderson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, Synthesis, and Structure−Activity Relationships of AminopyridineN-Oxides, a Novel Scaffold for the Potent and Selective Inhibition of p38 Mitogen Activated Protein Kinase

(2009) Wenceslao Lumeras et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel 2- and 4-Substituted 1H-Imidazo[4,5-c]quinolin-4-amine Derivatives as Allosteric Modulators of the A3Adenosine Receptor

(2009) Yoonkyung Kim et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly Efficient Borylation Suzuki Coupling Process for 4-Bromo-2-ketothiazoles: Straightforward Access to Micrococcinate and Saramycetate Esters

(2009) Thibaut Martin et al.   ORGANIC LETTERS

Synthesis of 4-Aryl-2-aminopyridine Derivatives and Related Compounds

(2009) Vladimir Pavlovic et al.   SYNTHETIC COMMUNICATIONS

Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors

(2008) Jun Tang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Enantioselective Total Synthesis of a β-Carboline Alkaloid, (S)-(−)-Dichotomine C

(2008) Kana Omura et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Design and synthesis of calpain inhibitory 6-pyridone 2-carboxamide derivatives

(2008) Ki Yong Lee et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Direct C-2 Arylation of Alkyl 4-Thiazolecarboxylates: New Insights in Synthesis of Heterocyclic Core of Thiopeptide Antibiotics

(2008) Thibaut Martin et al.   ORGANIC LETTERS

Synthesis of 2-aryl-6-methyl-5-nitroquinoline derivatives as potential prodrug systems for reductive activation

(2008) Gavin D. Couch et al.   TETRAHEDRON