Cu(I)-Catalyzed Trideuteromethylthiolation for the Synthesis of S-Methyl- d 3 Triazoles via an Interrupted Click Reaction

Abstract

Abstract Herein, we report a Cu(I)-catalyzed trideuteromethylthiolation reaction for the preparation of various S-methyl-d3 triazoles. This protocol proceeds via a Cu(I)-catalyzed azide–alkyne cycloaddition, followed by interception of the in situ-formed cuprate–triazole intermediate with S-(methyl-d3) 4-methylbenzenesulfonothioate. The reaction features excellent deuterium incorporation, mild conditions, and late-stage functionalization of bioactive molecules.