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

Organic & Biomolecular Chemistry Pub Date: 2023-05-03 DOI: 10.1039/D3OB00566F

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.

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