Base‐Promoted Formylation and N‐Difluoromethylation of Azaindoles with Ethyl Bromodifluoroacetate as a Carbon Source

Abstract

Main observation and conclusionWe 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.