Iridium(III)-Catalyzed One-Pot Access to 1,2-Disubstituted Benzimidazoles Starting from Imidamides and Sulfonyl Azides

A novel Ir-catalyzed annulation of imidamides with sulfonyl azides has been developed. 1,2-Disubstituted benzimidazoles could be easily obtained in up to 99% yield for more than 40 examples. The products further streamline the synthesis of molecules that are important building blocks for organic synthesis and drug discovery. This strategy features high regioselectivity, efficiency, good tolerance of functional groups, and mild reaction conditions.