铁粉促进“一锅法”合成1-苯基苯并咪唑类化合物

“One-Pot” Synthesis of 1-Phenyl-1H-benzimidazole Derivatives Facilitated by Fe

成功开发了由铁粉促进“一锅法”合成1-苯基苯并咪唑类化合物的简易合成方法,以取代邻硝基二苯胺为原料，液体有机酸为溶剂，在铁粉作用下还原并直接环合生成1-苯基苯并咪唑类化合物，产率80％-93％,通过高效液相色谱（HPLC）监测分析反应进程，探讨反应的机理，并确定了最佳反应条件．该合成方法条件温和，操作简单，原料易得，产率较高，为该类化合物的合成提供了一种新的便利方法．

An easy and efficient ＂one-pot＂ synthetic method facilitated by Fe to synthesize substituted 1-phenyl-lH-benzimidazole has been developed successfully. By using liquid organic acid as solvent, 2-nitro-N-phenylaniline is converted to sub- stituted 1-phenyl-1H-benzimidazole directly after reduction and cyclization catalyzed by Fe, with the yield of 80%-92%. Through the application of high performance liquid chromatography （HPLC） detection, the effects of the amount of solvent, the type of liquid organic acid, temperature and reaction time on the ＂one-pot＂ reaction have been fully investigated, as well as the reaction mechanism. The ＂one-pot＂ method proposed here has multiple advantages, such as mild condition, easy procedure, cheap ingredients and high yield, which provide a newly convenient synthetic route.