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酒石酸托特罗定的合成
引用本文:孙钦美,马淑涛,张贵民. 酒石酸托特罗定的合成[J]. 齐鲁药事, 2010, 29(5): 301-303
作者姓名:孙钦美  马淑涛  张贵民
作者单位:1. 山东大学药学院,山东,济南,250012
2. 鲁南制药集团股份有限公司,山东,临沂,276006
摘    要:
目的合成酒石酸托特罗定。方法以肉桂酸和对甲苯酚为起始原料,经环合、甲基化、还原、对甲苯磺酰化、胺化、脱甲基、拆分七步反应合成酒石酸托特罗定。结果与结论总收率为16.5%。该合成路线简洁,反应步骤少,适宜工业化生产。

关 键 词:酒石酸托特罗定  M-受体拮抗剂  药物合成

Synthetic of tolterodine tartrate
SUN Qin-mei,MA Shu-tao,ZHANG Gui-min. Synthetic of tolterodine tartrate[J]. qilu pharmaceutical affairs, 2010, 29(5): 301-303
Authors:SUN Qin-mei  MA Shu-tao  ZHANG Gui-min
Affiliation:(Shool of Pharmaceutical Sciences Shandong Univerisity,Ji'nan 250012;1.Lunan Pharmaceutical Group Limited Company,Linyi 276006)
Abstract:
OBJECTIVE To synthesis tolterodine L-tratrate.METHODS Tolterodine tartrate was synthesized through the cyclization,methylation,reduction,sulfonylation,amidation,demethylation,separation from the starting material Cinnamic acid and P-cresp.RESULTS and CONCLUSION The total yield of the target compound was 18.7%.The synthetic procedure was convenient and suitable for industrial manufacture.
Keywords:Tolterodine tartrate  M-receptor antagonist  synthesis
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