Mukaiyama reagent: An efficient reaction mediator for rapid synthesis of 1,2-disubstituted-1H-benzo[d]imidazoles

Within the field of medicinal chemistry, 1,2-disubstituted benzimidazoles represent a privileged class of nitrogen-based heterocycles but, unlike 2-substitued derivatives, few synthetic methods have been reported. In this context, we developed a rapid, metal-free, and straightforward method to prepare a series of 1,2-disubstituted-1H-benzo[d]imidazoles starting from 1,2-phenylendiamines and various aromatic and aliphatic aldehydes in the presence of the Mukaiyama reagent. The reaction proceeded at room temperature with good product yields within few minutes.