Catalyst-free C(sp3)–H functionalization of methyl azaarenes with heteroaromatic trifluoromethyl ketone hydrates: “all-water” synthesis of α-trifluoromethyl tertiary alcohols

Abstract

An efficient catalyst-free C(sp³)–H bond functionalization of methyl azaarenes with heteroaromatic trifluoromethyl ketone hydrates in neat water has been developed for the synthesis of α-trifluoromethyl tertiary alcohols bearing N-heteroaromatics. This method not only features excellent efficiency, broad substrate scope, catalyst-free conditions, and easy gram-scale preparation but also represents a new and rare example of “all-water” synthesis of trifluoromethylated molecules.