摘要
目的:优化盐酸雷洛昔芬的合成路线。方法:以3-甲氧基苯硫酚和4-甲氧基-α-溴代苯乙酮为起始原料,经取代反应,环合反应得到6-甲氧基-2-(4-乙酰氧基苯基)苯并[b]噻吩,再与4-[2-(1-哌啶基)乙氧基]苯甲酰氯盐酸盐发生Friedel-Crafts反应,然后发生脱甲基反应,最后经成盐反应,共5步主要反应制得目标产物。结果:目标化合物结构经红外光谱、核磁共振氢谱及质谱确证。结论:本方法反应条件温和,操作简便,并且提高了产率。
Objective：To optimize the synthetic route of raloxifene hydrochloride.Methods：The target compound was synthesized from 3- methoxybenzenethiol and 4- methoxy-α- bromo acetophenone via five steps, including substitution, cyclization, Friedel-Crafts reaction, demethyl reaction and salt formation. Results： The structure of the target compound was confirmed by IR, ^1 H-NMR and MS. Conclusion： This synthetic route had a mild reaction condition and improved yield,and was easily controlled.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2005年第7期882-884,共3页
Chinese Journal of New Drugs
