Process for the separation of the two optical isomers of 1-(o-methoxyphenoxy)-3-isopropylamino-propan-2-ol, optical isomers obtained thereby and pharmaceutical compositions of the levorotatory antipode thereof
申请人:SIMES S.p.A. Società
Italiana Medicinali e Sintetici
公开号:EP0015418A1
公开(公告)日:1980-09-17
A process for the separation of moprolol having formula (I) into its two optical antipodes, by salifying racemic moprolol with L(+)glutamic acid; treating the thus obtained mixture of diastereoisomeric salts with a water/alcohol mixture, in this way separating the L(+)glutamate insoluble salt of (+)moprolol; treating the resultant mother liquors which contain in solution the L(+)glutamate salt of (-)moprolol with a base so as to separate the levorotatory isomer of crystalline moprolol, which finally undergoes a purification.
Also a pharmaceutical composition containing said levorotatory isomer of moprolol.
一种将式(I)莫普洛尔分离为两种光学异构体的工艺,其方法是用 L(+)谷氨酸盐化外消旋莫普洛尔;用水/醇混合物处理由此获得的非对映异构盐混合物,从而分离出(+)莫普洛尔的 L(+)谷氨酸不溶性盐;用碱处理所得母液,母液溶液中含有(-)莫普洛尔的 L(+)谷氨酸盐,从而分离出结晶莫普洛尔的左旋异构体,最后进行纯化。
此外还有一种药物组合物,其中含有所述的莫普洛尔左旋异构体。