天然产物bistramide D螺缩酮片段的合成研究  

Synthesis of the spiroketal fragment of bistramide D

作　　者：李璐 郭湘立 邓涛 LI Lu;GUO Xiang-li;DENG Tao(Chemistry and Chemical Engineering Department,Tianjin Vocational Institute,Tianjin 300410,China)

机构地区：[1]天津职业大学生物与环境工程学院,天津300410

出　　处：《中国药物化学杂志》2021年第12期979-987,共9页Chinese Journal of Medicinal Chemistry

基　　金：天津市教委科研计划项目(2020KJ069);天津职业大学横向科研项目(60002/604046)。

摘　　要：目的以金离子催化环化反应为关键步骤合成天然产物bistramide D的螺缩酮片段。方法以手性噁唑烷酮为起始原料,通过汇集合成方法高效制备出关键中间体A和B,再经金离子催化环化等9步反应以14%总收率完成了bistramide D螺缩酮片段的合成。结果与结论Bistramide D螺缩酮的结构经^(1)H-NMR、^(13)C-NMR、IR和MS确证。该制备路线反应条件温和、收率好、选择性高。The spiroketal fragment of bistramide D has been successfully constructed in enantiomerically highly enriched form,featuring a Au(I) catalyzed dehydrative cyclization.The synthesis started from the readily available Evan′s oxazolidinone which lead to key intermediates A and B in a convergent fashion,then following 9 linear steps.The fragment was prepared in 14% overall yield.The molecular structure has been confirmed by ^(1)H-NMR,^(13)C-NMR,IR and MS.The synthetic route owns the highlights of mild reaction condition,good yielding and high selectivity.■.

关 键 词：bistramide D 螺缩酮 环化 金离子催化 

分 类 号：R914[医药卫生—药物化学]