Premium
Base‐Promoted Formylation and N ‐Difluoromethylation of Azaindoles with Ethyl Bromodifluoroacetate as a Carbon Source
Author(s) -
Li Yang,
Sun Ning,
Zhang CaiLin,
Hao Meng
Publication year - 2021
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.202100008
Subject(s) - chemistry , formylation , aldehyde , catalysis , combinatorial chemistry , organic chemistry
Main observation and conclusion We reported for the first time that ethyl bromodifluoroacetate directly reacts with azaindole without transition metal catalysis to produce a difluoromethyl protected 5‐aldehyde group product in one step. It is worth mentioning that the reacted aldehyde group is only formed at the 5 position. In addition, this method has good substrate applicability and functional group tolerance. Finally, we also carried out some mechanism auxiliary experiments, which confirmed that the aldehyde‐based carbon comes from ethyl bromo‐ difluoroacetate.