Synthesis of 1,2‐Disubstituted Benzimidazoles by a Cu‐Catalyzed Cascade Aryl Amination/Condensation Process

Helpful neighbors: A wide range of 1,2-disubstituted benzimidazoles can be assembled from 2-haloanilides and primary amines by using a copper-catalyzed amination reaction promoted by an ortho-substituent effect of an NHCOR group (see scheme, DMSO=dimethyl sulfoxide). The strategy also permits a broad array of substituents X at different positions of the benzimidazole phenyl ring.