Cu-Catalyzed One-Pot Synthesis of 1,2-Disubstituted Benzimidazoles

Significance

A practical copper-catalyzed one-pot synthesis of 1,2-disubstituted benzimidazoles and their derivatives is proposed. The ortho-substituent effect of the NHCOR functional groups allows for a regioselective amination in the first step of the reaction. Variations at the 1- and 2-positions can be easily achieved by using different primary amines and by diversifying the amido groups of the 2-haloacetanilides. In contrast to existing methods, this cascade reaction tolerates substituents at different positions of the benzimidazole phenyl ring.