抗肿瘤药物阿那曲唑的合成方法改进  

Improved synthetic method of anticancer drug anastrozole

作　　者：葛泽梅[1] 崔家玲[1] 程铁明[1] 李润涛[1] 

机构地区：[1]北京大学药学院,北京100083

出　　处：《中国药物化学杂志》2003年第3期146-147,152,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进抗肿瘤药物阿那曲唑的合成工艺。方法以 1,3,5 三甲苯为起始原料 ,经过两步溴化、氰化、甲基化和N 烷基化 5步反应合成阿那曲唑 ,在第二步和最后一步反应中使用相转移催化方法。结果成功地合成阿那曲唑 ,总收率为 2 8%。结论改进后的合成方法反应时间明显缩短 ,操作方法大大简化 ,所有原料均国产化 ,更适合于工业化生产。Aim To improve the synthetic procedure of the anticancer drug anastrozole.Method 1,3,5-trimethylbenzene was selected as the start material.The final product was obtained in five steps,including two steps bromination,cyanidation,methylation and N -alkylation.Result Anastrozole has been synthesized in the total yield 28%.Conclusion The phase transfer catalyst method was successfully used in step 2 and 5.Compared with the patent method,the operation was simplified,the reaction time was shortened,all the materials can be obtained from our country and are more suitable for preparing it on a large scale.

关 键 词：药物化学 制备 化学合成 相转移催化 阿那曲唑 抗肿瘤 

分 类 号：R914[医药卫生—药物化学]