A simple and efficient approach to the synthesis of 2-substituted benzimidazole via sp3 C-H functionalization

A facile and novel approach to the synthesis of 2-substituted benzimidazole was developed via a tandem reaction following sp3 C-H functionalization. Here we report a simple, efficient and tandem oxidative dehydrative coupling reaction of N-benzylbezene-1,2-diamine in the presence of oxidant tert-butyl hydroperoxide (TBHP) in solvent acetonitrile to give substituted benzimidazole.