Molecules

Aqueous synthesis of 1-H-2-substituted benzimidazoles via transition-metal-free intramolecular amination of aryl iodides

C Chen, C Chen, B Li, J Tao, J Peng

Index: Chen, Chunxia; Chen, Chen; Li, Bin; Tao, Jingwei; Peng, Jinsong Molecules, 2012 , vol. 17, # 11 p. 12506 - 12520

Full Text: HTML

Citation Number: 14

Abstract

Abstract A straightforward method has been developed for the synthesis of the benzimidazole ring system through a carbon-nitrogen cross-coupling reaction. In the presence of 2.0 equiv. of K 2 CO 3 in water at 100 C for 30 h, the intramolecular cyclization of N-(2-iodoaryl) benzamidine provides benzimidazole derivatives in moderate to high yields. Remarkably, the procedure occurs exclusively in water and doesn't require the use ...