Department of Chemistry, Institute of Basic Science, Chonnam National University, 300 Yongbong-dong, Buk-gu, Gwangju 500-757, Republic of Korea.
J Org Chem. 2011 Dec 2;76(23):9577-83. doi: 10.1021/jo2019416. Epub 2011 Nov 8.
Benzimidazoles were synthesized by the copper-catalyzed, one-pot, three-component reaction of 2-haloanilines, aldehydes, and NaN(3). The reaction was optimized when 2-iodo- or 2-bromoanilines (1.0 equiv), aldehydes (1.2 equiv), NaN(3) (2.0 equiv), 5 mol% of CuCl, and 5 mol % of TMEDA were reacted in DMSO at 120 °C for 12 h. Good yields resulted, and the reaction showed tolerance toward functional groups such as ester, nitro, and chloro. Aliphatic and heteroaromatic aldehydes also afforded the desired products in moderate to good yields.
苯并咪唑类化合物可通过 2-卤代苯胺、醛和NaN3 的铜催化一锅、三组分反应合成。当 2-碘代或 2-溴代苯胺（1.0 当量）、醛（1.2 当量）、NaN3（2.0 当量）、5 mol%的 CuCl 和 5 mol%的 TMEDA 在 DMSO 中于 120°C 反应 12 小时时，反应得到了优化。产率良好，并且该反应对酯、硝基和氯等官能团具有耐受性。脂肪族和杂芳醛也以中等至良好的收率得到了所需的产物。
