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. (C) 2022 Elsevier Ltd. All rights reserved.

Automated summary

This article presents a rapid, metal-free, and straightforward method for synthesizing a series of 1,2-disubstituted-1H-benzo[d]imidazoles.