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Catalytic Enantioselective α‐Fluorination of 2‐Acyl Imidazoles via Iridium Complexes
Author(s) -
Xu GuoQiang,
Liang Hui,
Fang Jie,
Jia ZhiLong,
Chen JianQiang,
Xu PengFei
Publication year - 2016
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201601306
Subject(s) - enantioselective synthesis , iridium , catalysis , combinatorial chemistry , substrate (aquarium) , chemistry , fluorine , organic chemistry , prodrug , biochemistry , oceanography , geology
The first highly enantioselective α‐fluorination of 2‐acyl imidazoles utilizing iridium catalysis has been accomplished. This transformation features mild conditions and a remarkably broad substrate scope, providing an efficient and highly enantioselective approach to obtain a wide range of fluorine‐containing 2‐acyl imidazoles which are found in a variety of bioactive compounds and prodrugs. A large scale synthesis has also been tested to demonstrate the potential utility of this fluorination method.