Li Zhaoguang, Sun Hongbin, Jiang Hualiang, Liu Hong
Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Org Lett. 2008 Aug 7;10(15):3263-6. doi: 10.1021/ol8011106. Epub 2008 Jul 2.
An efficient and convenient method was developed for preparing N-substituted 1,3-dihydrobenzimidazol-2-ones from N'-substituted N-(2-halophenyl)ureas via a CuI/DBU-catalyzed cyclization in DMSO under microwave heating. High yields were obtained and a variety of functional groups were tolerated under these conditions, including N'-aryl, alkyl, heterocyclic, various N-(substituted 2-halophenyl) and N-(2-iodopyridyl)ureas.
开发了一种高效便捷的方法，通过在微波加热下，在二甲基亚砜（DMSO）中由碘化亚铜（CuI）/ 1,8-二氮杂二环[5.4.0]十一碳-7-烯（DBU）催化环化反应，从N'-取代的N-(2-卤代苯基)脲制备N-取代的1,3-二氢苯并咪唑-2-酮。在这些条件下获得了高产率，并且各种官能团都能耐受，包括N'-芳基、烷基、杂环、各种N-(取代的2-卤代苯基)和N-(2-碘吡啶基)脲。
