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发明公开
CN1903833A 一种制备托特罗定及其L－酒石酸盐的方法 失效 - 权利终止

一种制备托特罗定及其L－酒石酸盐的方法
摘要：
本发明公开了一种托特罗定及其L－酒石酸盐的制备方法，其步骤是：由对甲酚和肉桂酸制备出6－甲基－4－苯基－3，4－二氢香豆素，进一步制得3－(2－羟基－5－甲基苯基)－3－苯基丙醇，进一步制得3－(2－羟基－5－甲基苯基)－3－苯基卤代丙烷进一步制得3－(2－羟基保护基－5－甲基苯基)－3－苯基卤代丙烷，进一步制得N，N－二异丙胺－3－(2－羟基保护基－5－甲基苯基)－3－苯基丙胺，最后得到消旋的托特罗定(I)。用L－(+)－酒石酸拆分消旋托特罗定I，制得L－(+)－酒石酸－R－托特罗定。本发明操作简便，无需使用四氢铝锂或DIBAL－H等还原试剂，反应产率高，成本低，工艺稳定，适合工业化生产。
摘要（英）：

The present invention discloses a preparation method of thoterodine and its L-tartrate. Said preparation method includes the following steps: using paracresol and cinnamic acid to prepare 6-methyl-4-phenyl-3,4-coumaran, using it to further prepare 3-(2-hydroxy-5-methylphenyl)-3-phenylpropanol, further preparing 3-(2-hydroxy-5-methylphenyl)-3-phenyl halogenated propane, then further preparing 3-(2-hydroxy protecting group-5-methylphenyl)-3-phenyl halogenated propane, and further preparing N,N-diisopropylamine-3-(2-hydroxy protecting group-5-methylphenyl)-3-phenylprophlamine, finally obtaining racemic thoterodine, then using L-(t)-tartaric acid to resolve racemic thoterodine so as to obtain L-(+)-tarlaric acid-R-thoterodine.

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