Fluorination methods in drug discovery

DE Yerien, S Bonesi, A Postigo - Organic & Biomolecular Chemistry, 2016 - pubs.rsc.org
Fluorination reactions of medicinal and biologically-active compounds will be discussed.
Late stage fluorination strategies of medicinal targets have recently attracted considerable …

Advances in dearomatization strategies of indoles

SP Roche, JJY Tendoung, B Treguier - Tetrahedron, 2015 - Elsevier
Over the years, alkaloids derived from indole dearomatization, such as indolenine and
indolines have been evolved as promising therapeutic agents due to their important …

Amide-assisted radical strategy: Metal-free direct fluorination of arenes in aqueous media

D Liang, Y Li, S Gao, R Li, X Li, B Wang, H Yang - Green Chemistry, 2017 - pubs.rsc.org
A metal-and initiator-free direct fluorination of arenes with the assistance of an amide group
is developed. This reaction proceeded under simple aqueous conditions with good …

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

P Chen, G Liu - European Journal of Organic Chemistry, 2015 - Wiley Online Library
Direct aminofluorination of alkenes enables the convenient synthesis of β‐fluorinated amine
compounds, which are important and valuable skeletons in medicinal chemistry. In recent …

Ring-opening fluorination of bicyclic azaarenes

M Komatsuda, A Suto, H Kondo, H Takada, K Kato… - Chemical …, 2022 - pubs.rsc.org
We have discovered a ring-opening fluorination of bicyclic azaarenes. Upon treatment of
bicyclic azaarenes such as pyrazolo [1, 5-a] pyridines with electrophilic fluorinating agents …

Synthesis of 3-selanylbenzo [b] furans promoted by SelectFluor®

MCDF Xavier, EMA Sandagorda, JSS Neto… - RSC …, 2020 - pubs.rsc.org
A simple and practical protocol for the synthesis of 3-selanyl-benzo [b] furans mediated by
the SelectFluor® reagent was developed. This novel methodology provided a greener …

Enantioselective Cascade Michael/Hemiaminal Formation of α,β-Unsaturated Iminoindoles with Aldehydes Using a Chiral Aminomethylpyrrolidine Catalyst Bearing a SO2C6F …

K Moriyama, Y Oka - ACS Catalysis, 2022 - ACS Publications
An enantioselective cascade Michael/hemiaminal formation of α, β-unsaturated
iminoindoles with aldehydes using a chiral aminomethylpyrrolidine catalyst bearing a …

Rhodium (III)-catalyzed regioselective C2-amidation of indoles with N-(2, 4, 6-trichlorobenzoyloxy) amides and its synthetic application to the development of a novel …

J Shi, G Zhao, X Wang, HE Xu, W Yi - Organic & biomolecular …, 2014 - pubs.rsc.org
A new and efficient method for the direct regioselective C2-amidation of various
functionalized indoles with several N-(2, 4, 6-trichlorobenzoyloxy) amides via Rh (III) …

Synthesis of 2‐Oxindoles from Substituted Indoles by Hypervalent‐Iodine Oxidation

X Jiang, C Zheng, L Lei, K Lin… - European Journal of …, 2018 - Wiley Online Library
A practical conversion of indoles into the corresponding 2‐oxindoles is achieved efficiently
using a hypervalent iodine reagent. This oxidation is amenable to different substituted …

Amination/cyclization cascade by acid-catalyzed activation of indolenine for the one-pot synthesis of phaitanthrin E

T Abe, K Yamada - Organic letters, 2016 - ACS Publications
Amination/Cyclization Cascade by Acid-Catalyzed Activation of Indolenine for the One-Pot
Synthesis of Phaitanthrin E | Organic Letters ACS ACS Publications C&EN CAS Find my …