首页> 外国专利> IMPROVED PROCESS FOR ISOLATING DESIRED ISOMERS OF NEBIVOLOL INTERMEDIATES AND USE THEREOF FOR THE PREPARATION OF NEBIVOLOL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

IMPROVED PROCESS FOR ISOLATING DESIRED ISOMERS OF NEBIVOLOL INTERMEDIATES AND USE THEREOF FOR THE PREPARATION OF NEBIVOLOL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

机译:分离所需的奈必洛尔中间体异构体的改进方法,并将其用于制备奈必洛尔或可药用盐

摘要

FIELD OF THE INVENTION Disclosed herein is an improved, commercially viable and industrially advantageous process for the separation of desired isomers of nebivolol intermediates from a mixture containing desired and undesired isomers of nebivolol intermediates. The desired isomers of nebivolol intermediates are useful for preparing nebivolol, or a pharmaceutically acceptable salt thereof in high yield and purity. BACKGROUND OF THE INVENTION EP Patent No. 0145067 discloses a variety of 2,2'-iminobisethanol derivatives. These compounds are antihypertensive agents. Of these compounds, nebivolol is a racemic mixture of RSSS and its enantiomer of a,a'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol], and the structures of these isomers are shown below with stereo chemical notation at each chiral centre.
机译:发明领域本文公开了一种改进的,商业上可行的且工业上有利的方法,用于从含有奈必洛尔中间体的所需和不希望的异构体的混合物中分离奈必洛尔中间体的所需异构体。奈必洛尔中间体的所需异构体可用于以高收率和纯度制备奈必洛尔或其药学上可接受的盐。发明背景欧洲专利第0145067号公开了各种2,2′-亚氨基双乙醇衍生物。这些化合物是抗高血压药。在这些化合物中,奈比洛尔是RSSS与a,a'-[亚氨基双(亚甲基)]双[6-氟-3,4-二氢-2H-1-苯并吡喃-2-甲醇]的对映异构体的外消旋混合物,并且这些异构体的结构如下所示,在每个手性中心带有立体化学符号。

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