Aqueous Synthesis of 1-H-2-Substituted Benzimidazoles via Transition-Metal-Free Intramolecular Amination of Aryl Iodides

作者：Chen Chunxia; Chen Chen; Li Bin^*; Tao Jingwei; Peng Jinsong

来源：Molecules, 2012, 17(11): 12506-12520.

DOI：10.3390/molecules171112506

• benzimidazoles
• aqueous synthesis
• N-arylation
• transition-metal-free conditions
• aryl iodides

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 K2CO3 in water at 100 degrees 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 of any additional reagent/catalyst, rendering the methodology highly valuable from both environmental and economical points of view.

• 出版日期2012-11
• 单位东北林业大学