佐米曲普坦的合成及工艺改进  

Improvement of synthesis technology of zolmitriptan

作　　者：张玲[1] 曲有乐[2] 周淑晶[1] 

机构地区：[1]佳木斯大学化学与药学院,黑龙江佳木斯154007 [2]浙江海洋学院,浙江定海316000

出　　处：《黑龙江医药科学》2006年第2期32-33,共2页Heilongjiang Medicine and Pharmacy

摘　　要：目的:改进佐米曲普坦的合成工艺。方法:以(L)-苯丙氨酸为原料,经硝化,酯化,还原(酯基),环合,还原(硝基),重氮化,还原(重氮盐)和费歇尔吲哚合成共八步反应制得佐米曲普坦。结果:改进了佐米曲普坦的合成工艺,总收率提高至16%。结论:改进后的合成工艺操作简便,成本低,收率高,适于工业化生产。Objective： To improve the synthesis technology of zolmitriptan. Method： Zolmitriptan was synthesized from L - pheneylalanine via nitration, esterfication, reduction （ - COOR）, cylization, - NO2 reduction, diazotization, diazonium salt reduction and fischer indole synthesis. Results： We successfully improved the synthesis technology of zolmitriptan with an overall yield of 16%. Conclusion ：The improved synthesis technology has many advantages,such as more convenient operation ,lower cost ,higher yield, suitble for its industrialized production.

关 键 词：佐米曲普坦 抗偏头痛药 合成 

分 类 号：R914.5[医药卫生—药物化学]