Synthesis of Methyl-d3 Arene via Electrochemical Deuterodefluorination of Trifluoromethyl Arene.

Abstract

The methyl-d3 group is a new isotopic functional group for medicine design. In this work, we report an electrochemical deuteration approach for converting aromatic trifluoromethyl to methyl-d3 groups with deuterium water in common DMF. Yields up to 94%, D ratio up to 97%, and CD3 incorporation up to 90% were achieved. A basic additive is the key factor enabling the highly chemoselective reaction.