DOI: 10.1055/s-0036-1590915
short review
© Georg Thieme Verlag Stuttgart · New York

Recent Advances in the Synthesis of Benzimidazole Derivatives from the Oxidative Coupling of Primary Amines

Martine Largeron*, Khac Minh Huy Nguyen
  • UMR 8638 CNRS-Université Paris Descartes (Paris 5), Sorbonne Paris Cité, Faculté de Pharmacie de Paris, 4 avenue de l’Observatoire, 75270 Paris cedex 06, France   Email:
Further Information

Publication History

Received: 30 August 2017

Accepted after revision: 01 September 2017

Publication Date:
21 September 2017 (eFirst)


Benzimidazole belongs to the top five most commonly used five-membered aromatic nitrogen heterocycles among U.S. FDA approved pharmaceuticals. Over the last few years, a large number of improved synthetic strategies have been developed to construct the benz­imidazole molecular framework under environmentally benign conditions. This review focuses on the use of primary amines as readily available substrates for the synthesis of benzimidazole derivatives through different types of oxidative cross-coupling reactions.

1 Introduction

2 Catalyst-Free Oxidative Coupling of Primary Amines

3 Catalytic Oxidative Coupling of Primary Amines

3.1 Metal-Catalyzed Reactions

3.2 Metal-Free Catalyzed Reactions

3.3 Bioinspired Catalyzed Reactions

4 Conclusion