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.