Transition-Metal-Free N-Functionalization of Benzimidazoles and Related Azaheterocycles with α-Acyloxy Sulfides

Direct N-functionalization of benzimidazoles and related azaheterocycles has been achieved using readily accessible alpha-acyloxy sulfides under transition metal-free conditions. In the presence of the base, potassium carbonate, a variety of N-functionalized azaheterocyclic compounds bearing an N-alkyl ester moiety were synthesized from corresponding heterocyclic precursors. The present reaction does not use transition metals, is operationally simple, and has broad substrate scope.

Automated summary

Direct N-functionalization of benzimidazoles and related azaheterocycles was achieved using readily accessible alpha-acyloxy sulfides under transition metal-free conditions. The reaction is operationally simple and has a broad substrate scope.