Premium
Dehydroxylative Trifluoromethylthiolation, Trifluoromethylation, and Difluoromethylation of Alcohols
Author(s) -
Zhang Wei,
Lin JinHong,
Wu Wenfeng,
Cao YuCai,
Xiao JiChang
Publication year - 2020
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201900364
Subject(s) - trifluoromethylation , chemistry , scope (computer science) , functional group , combinatorial chemistry , substrate (aquarium) , halogenation , organic chemistry , medicinal chemistry , trifluoromethyl , alkyl , oceanography , computer science , programming language , geology , polymer
Summary of main observation and conclusion CF 3 S, CF 3 and HCF 2 groups have been identified as valuable functionalities for drug development. Despite significant accomplishments in the trifluoromethylthiolation, trifluoromethylation and difluoromethylation reactions, directly converting common functional groups into CF 3 S, CF 3 or HCF 2 groups is still highly desirable. Described here is the dehydroxylative trifluoromethylthiolation, trifluoromethylation and difluoromethylation of alcohols promoted by a R 3 P/ICH 2 CH 2 I system. All of these dehydroxylative reactions were achieved under mild conditions via the activation of the hydroxyl group by the R 3 P/ICH 2 CH 2 I system. A wide substrate scope and good functional group tolerance were observed.