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A process for the purification and isolation of an optically active atenolol with a high yield

机译:以高收率纯化和分离光学活性阿替洛尔的方法

摘要

PURPOSE:To selectively obtain an optically active atenolol salt having high solubility from atenolol salt having low optical purity by treating a salt comprising atenolol and Bronsted acid with solvent. CONSTITUTION:An atenolol salt comprising atenolol and a Bronsted acid (e.g. hydrohalogenic acid, sulfuric acid, phosphoric acid or carboxylic acid, sulfonic acid or phenol which contains 2-17C alkyl, aralkyl or aryl group) is treated with a proper solvent by taking advantage of difference in solubility between racemic modification and optical active substance of the atenolol salt, an optically active atenolol salt having high optically activity is selectively taken out and the acid component is removed from the atenolol salt to give optically active atenolol. A method of extracting optically active salt from solid content of atenolol salt by using a solvent or a method of dissolving the atenolol salt in a solvent, precipitating a solid having high content of racemic modification salt, subjecting to solid-liquid separation and collecting the optically active salt from the solution part may be cited as the treating method.
机译:目的:通过用溶剂处理包含阿替洛尔和布朗斯台德酸的盐,从光学纯度低的阿替洛尔盐中选择性地获得具有高溶解度的光学活性阿替洛尔盐。组成:包含阿替洛尔和布朗斯台德酸(例如氢卤代酸,硫酸,磷酸或羧酸,磺酸或苯酚中含有2-17C烷基,芳烷基或芳基)的阿替洛尔盐可通过以下方法用适当的溶剂处理:对于阿替洛尔盐的外消旋修饰物和旋光活性物质之间的溶解度差,选择具有高光学活性的旋光性阿替洛尔盐,并从阿替洛尔盐中除去酸成分,得到旋光性阿替洛尔。一种通过使用溶剂从阿替洛尔盐的固体含量中提取旋光性盐的方法,或者是将阿替洛尔盐溶解在溶剂中,沉淀出具有高含量外消旋改性盐的固体,进行固液分离并光学收集的方法。来自溶液部分的活性盐可以作为处理方法。

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