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 reactions 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.