Rh(iii)-catalyzed cascade C–H activation/amination enables the synthesis of 1,2-disubstituted benzimidazoles from amidines and arynes

Abstract

Benzimidazoles are versatile and indispensable scaffolds widely used in organic synthesis. Herein, we report a Rh(III)-catalyzed cascade C–H activation/amination reaction between amidines and arynes, enabling the efficient synthesis of 1,2-disubstituted benzimidazoles. This protocol features excellent functional group tolerance and moderate to high product yields.