State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences , Beijing 100050, P.R. China.
Department of Medicinal Chemistry, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences , Beijing 100050, P.R. China.
J Org Chem. 2018 Feb 2;83(3):1387-1393. doi: 10.1021/acs.joc.7b02894. Epub 2018 Jan 17.
An efficient and facile method has been developed for the diversity-oriented synthesis of heterocycles. Hexahydrophenoxazines, tetrahydroquinolines, indolines, hexahydrocarbazoles, and lactones were conducted via Al(OTf)-promoted cascade cyclization and ionic hydrogenation. Furthermore, this protocol was utilized to smoothly prepare piracetam and its key intermediate as well.
一种高效、简便的方法已经被开发用于杂环化合物的多样性导向合成。通过 Al(OTf)促进的级联环化和离子氢化，可以合成六氢苯并恶嗪、四氢喹啉、吲哚啉、六氢咔唑和内酯。此外，该方案还被用于顺利制备吡拉西坦及其关键中间体。
