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酒石酸托特罗定的合成研究
引用本文:王景阳,黄淑云,张增均. 酒石酸托特罗定的合成研究[J]. 天津药学, 2006, 18(5): 71-73
作者姓名:王景阳  黄淑云  张增均
作者单位:天津药物研究院,天津,300193
摘    要:
目的:合成酒石酸托特罗定并进行工艺改进。方法:以对甲苯酚为起始原料,经缩合、甲基化、还原、酯化、胺化、脱甲基化、拆分、精制等反应合成酒石酸托特罗定,并对脱甲基化反应进行了工艺改进。结果:通过改进工艺,总收率由9.23%提高到13.5%。结论:优化工艺后,收率提高,成本降低,解决了劳动保护和环保问题,更适合工业化生产。

关 键 词:酒石酸托特罗定  合成工艺  毒蕈碱受体拮抗剂
文章编号:1006-5687(2006)05-0071-03
收稿时间:2006-06-30
修稿时间:2006-06-30

Synthesis of tolterodine L-tartrate
Wang Jingyang,Huang Shuyun,Zhang zengjun. Synthesis of tolterodine L-tartrate[J]. Tianjin Pharmacy, 2006, 18(5): 71-73
Authors:Wang Jingyang  Huang Shuyun  Zhang zengjun
Affiliation:Tianjin Institute of Pharmaceutical Reserch, Tianjin 300193
Abstract:
Object: To synthesis tolterodine L-tartrate and improve the synthetic technology.Methods: Tolterodine was synthesized through the condensation,methylation,reduction,esterification,ammoniation,demethylation,sepration from the stating material p-methylphenol.The condition of demethylation was improved.Results: The overall yield increased from 9.23% to 13.5% with improved technology.Conclusion: The improved technology with higher overall yield and lower costs was more suitable for industry production.
Keywords:tartrate  tolterodine  synthesis  antimuscarinic agent
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