College of Chemistry , Fuzhou University , Fuzhou , Fujian 350116 , China.
Org Lett. 2018 Sep 7;20(17):5457-5460. doi: 10.1021/acs.orglett.8b02377. Epub 2018 Aug 23.
Herein, we report a biomimetic oxidative coupling cyclization strategy for the highly efficient functionalization of tetrahydrocarbolines (THCs). This process enables rapid access to complex isochromanoindolenine scaffolds in moderate to excellent yields. The reaction proceeds smoothly and rapidly (complete within minutes) in an open flask. This operationally simple protocol is scalable and compatible with a wide range of functional groups. Late-stage functionalization of a pharmacologically relevant molecule is also demonstrated.
本文报道了一种仿生氧化偶联环化策略，可高效实现四氢咔啉（THCs）的功能化。该反应以中等至优秀的收率快速构建复杂的异吲哚并吲哚啉骨架。反应在开放烧瓶中平稳、快速（几分钟内完成）进行。该操作简单的方案具有可扩展性，并且与广泛的官能团兼容。还展示了对具有药理相关性的分子的后期功能化。
