Synthesis of axially chiral N-aryl benzimidazoles via chiral phosphoric acid catalyzed enantioselective oxidative aromatization

Abstract

Given the great importance of N-substituted benzimidazoles in pharmaceutics, here N-aryl benzimidazoline produced in situ was used as a H₂ donor, which was converted to C–N axially chiral N-aryl benzimidazole by CPA-catalyzed enantioselective transfer hydrogenation of the in situ produced imine.