Department of Chemistry and Chemical Engineering, College of Science, Northeast Forestry University, Harbin, 150040, PR China.
J Org Chem. 2011 Jan 21;76(2):716-9. doi: 10.1021/jo1021426. Epub 2010 Dec 22.
A straightforward, efficient, and more sustainable copper-catalyzed method has been developed for intramolecular N-arylation providing the benzimidazole ring system. With Cu(2)O (5 mol %) as the catalyst, DMEDA (10 mol %) as the ligand, and K(2)CO(3) as the base, this protocol was applied to synthesize a small library of benzimidazoles in high yields. Remarkably, the reaction was exclusively carried out in water, rendering the methodology highly valuable from both environmental and economical points of view.
一种简单、高效、更可持续的铜催化方法已被开发用于分子内 N-芳基化,提供苯并咪唑环体系。以 Cu(2)O(5mol%)为催化剂、DMEDA(10mol%)为配体、K(2)CO(3)为碱,该方案应用于以高产率合成了一系列苯并咪唑的小分子库。值得注意的是,该反应仅在水中进行,从环境和经济角度来看,该方法具有很高的价值。