General Synthesis of 1‐Substituted 2‐Methylbenzimidazoles from Ketones and 2‐Aminoacetanilide

Abstract

A novel method for preparation of 1‐substituted benzimidazoles via reductive amination of ketones with N‐differentiated 1,2‐diaminobenzenes is described. The method appears to be general in application to acyclic and cyclic ketones, as well as heteroatom‐substituted cyclic ketones.

Keywords:

• benzimidazoles
• reductive amination
• cyclization

Acknowledgments

We gratefully acknowledge helpful discussions with Alan Millar, William J. Smith, Elie A. Tabet, and Shiping Xie.