申请人:Mora, Paolo Corvi
公开号:EP0045918A1
公开(公告)日:1982-02-17
A process is taught for the synthesis of vincamine and related indole alkaloids, according to which, through only two steps and through a novel synthesis intermediate, namely the glycidic ester, having the formula
wherein R" represents -COOCH3 or -COOCH2CH3, 1-ethyl-1,2,3,4,5,6,7,12b-octahydroindole- [2,3-a] -quinolizine-1-carbaldehyde is reacted with a haloester in the presence of a base and the glycidic ester is converted to vincamine or apovincamine or like esters by reaction with a Lewis acid or a mineral acid, the reaction products being subsequently separated by chromatography.
本发明提出了一种合成长春胺和相关吲哚生物碱的工艺,根据该工艺,只需两个步骤,通过一种新型合成中间体,即具有式中 R "代表-COOCH3或-COOCH2CH3的缩水甘油酯,1-乙基-1,2,3,4,5,6,7,12b-八氢吲哚-[2,3-a] -喹嗪-1-甲醛在碱存在下与卤代酯反应,缩水甘油酯通过与路易斯酸或矿物酸反应转化为长春胺或阿朴长春胺或类似酯,反应产物随后通过色谱法分离。