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METHOD FOR SELECTIVE SEPARATION OF SALBUTAMOL RACEMIC MIXTURE

机译:沙丁胺醇类药物混合物的选择性分离方法

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to the chemical and pharmaceutical industry and is a method for the selective separation of a racemic mixture of salbutamol by a supercritical fluid chromatography method, which consists in separating the racemic mixture of salbutamol by elution using a mobile phase of supercritical CO2, alcohol and dynamic modifier from a solution of the racemic mixture of salbutamol in alcohol using a column consisting of silica gel with a chiral selector grafted to it, characterized in that salbutamol salt is used as the racemic mixture of salbutamol, the macrocyclic glycopeptide eremomycin is used as a chiral selector, and also by the fact that a dynamic modifier in the concentration of 10÷200 mM with respect to alcohol, consisting either of a mixture of isopropylamine with trifluoroacetic acid in a molar ratio of 1:1÷3:1, either from a mixture of isopropylamine with ammonium acetate in a molar ratio of 1:1÷5:1, while methanol is used as the alcohol, the separation is carried out at a temperature of 18÷25 °C.;EFFECT: invention allows the racemic salbutamol salt mixture to be separated in a single step to obtain the salt of R-salbutamol.;1 cl, 3 dwg, 3 ex
机译:发明领域本发明涉及化学和制药工业,并且是一种通过超临界流体色谱法选择性分离沙丁胺醇外消旋混合物的方法,该方法包括使用流动相通过洗脱分离沙丁胺醇的外消旋混合物。用硅胶和接枝有手性选择剂的硅胶柱从沙丁胺醇的外消旋混合物的醇溶液中提取超临界CO 2 ,醇和动态改性剂的相,其特征在于使用了沙丁胺醇盐作为沙丁胺醇的外消旋混合物,大环糖肽埃雷霉素被用作手性选择剂,并且由于相对于醇浓度为10÷200 mM的动态改性剂,由异丙胺与三氟乙酸的混合物组成摩尔比为1:1÷3:1的异丙胺与乙酸铵的混合物(摩尔比为1:1÷5:1),而甲醇用作醇,分离是在18÷25°C的温度下进行的;效果:本发明使外消旋沙丁胺醇盐混合物可以一步分离,得到R-沙丁胺醇盐; 1 cl,3 dwg, 3前

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