表鬼臼毒素的合成工艺改进  

Improvement of the Synthetic Route of Epipodophyllotoxin

作　　者：王美慧[1] 王桂艳[1] 王旭[1] 杨兆柱[1] 杜永祥[1] 

机构地区：[1]佳木斯大学药学院,佳木斯154007

出　　处：《天然产物研究与开发》2013年第12期1722-1725,1730,共5页Natural Product Research and Development

基　　金：黑龙江省教育厅科研项目(12521563);佳木斯大学科研项目(L2011-019)

摘　　要：本实验的研究目的在于设计表鬼臼毒素合成的新工艺。以2-烯-1,4-丁二醇为原料经克莱森重排、酯交换反应、羟醛缩合反应、傅克烷基化反应、Heck反应、氧化反应和还原反应等九步合成了表鬼臼毒素,总收率为4.39%,并通过质谱﹑核磁共振氢谱和核磁共振碳谱鉴定目标化合物的结构,HPLC检测纯度达到97.59%。The aim of this study was to improve the synthetic route for the synthesis of epipodophyllotoxin. Epipodophyl- lotoxin was synthesized from 2-alkene-1,4-diols by a nine-step reaction, including Ctaisen rearrangement reaction, trans- esterification, Aldol reaction, Friedel-Crafts aikylation, Heck reaction, oxidation and reduction. The total yield of epipodo- phyllotoxin was 4.39%. The structure was confirmed by MS,＇ H NMR and ,3 C NMR. The purity was up to 97.59% by HPLC.

关 键 词：表鬼臼毒素 臭氧氧化 合成 工艺改进 

分 类 号：R914.5[医药卫生—药物化学]