奥洛他定的合成  

Synthesis of a new H_1 receptor antagonist olopatadine

作　　者：刘雅茹[1] 冯雪松[1] 孟繁浩[1] 

机构地区：[1]中国医科大学药学院药物化学教研室,沈阳110001

出　　处：《中国新药杂志》2006年第23期2045-2046,共2页Chinese Journal of New Drugs

摘　　要：目的:合成新型H1受体阻滞剂奥洛他定。方法:以对羟基苯乙酸和苯酞为原料,经取代、环合、维蒂希反应等9步反应合成目标产物。结果与结论:合成了目标产物,其结构经MS和1H-NMR确定。Objective： To synthesize a new H1 receptor antagonist olopatadine. Methods： Starting from 4-hydroxyphenylacetic acid and pthalide, olopatadine hydrochloride was synthesized via nine synthetic route, such as nucleophilic, substitution, cyclization and Wittig reaction. Results： The structure of the target compound was confirmed by MS and t H-NMR. Conclusion： Olopatadine was obtainable by this synthetic route.

关 键 词：奥洛他定 H1受体阻滞剂 抗过敏 

分 类 号：R976[医药卫生—药品]