L-酒石酸托特罗定的合成  

Synthesis of tolterodine L-tartrate

作　　者：张小华[1] 李璟[1] 魏顺金 齐广辉[1] 

机构地区：[1]河北化工医药职业技术学院,石家庄050026 [2]河北化工研究院,石家庄050031

出　　处：《中国新药杂志》2007年第22期1895-1897,共3页Chinese Journal of New Drugs

摘　　要：目的:合成L-酒石酸托特罗定。方法:以肉桂酸和对甲酚为起始原料,经环和、甲基化、对甲苯磺酸酯化、胺化、脱甲基、拆分得到目标化合物。结果和结论:总收率为14.3%。其结构经1H-NMR确认。该合成路线简洁,反应步骤少,工艺条件温和,适宜工业化生产。Objective：To synthesize tolterodine L-tartrate . Methods：The target compound was synthesized from cinnamic acid and 4-methylphenol as starting agent via several steps including cyclization, methylation, p-toluenesulfonation, amination, demethylation, resolution. Result and Conclusion ： The total yield of the target compound was 14.3%. The structure was verified using ^1H-NMR . The synthetic procedure was convenient and mild for industrial manufacture.

关 键 词：L-酒石酸托特罗定 尿失禁 M受体阻滞剂 药物合成 

分 类 号：R983.1[医药卫生—药品]