首页> 外国专利> Process for the preparation of a therapeutically useful pure, more polar diastereomer of (6R, 7R) -7- 2- (2-aminothiazol-4-yl) -2 (Z) - (methoxyimino) acetamido -3- (methoxymethyl) -3-kefem-4-carboxylic acid-1- (isopropoxycarbonyloxy) ethyl ester

Process for the preparation of a therapeutically useful pure, more polar diastereomer of (6R, 7R) -7- 2- (2-aminothiazol-4-yl) -2 (Z) - (methoxyimino) acetamido -3- (methoxymethyl) -3-kefem-4-carboxylic acid-1- (isopropoxycarbonyloxy) ethyl ester

机译:(6R,7R)-7- [2-(2-氨基噻唑-4-基)-2(Z)-(甲氧基亚氨基)乙酰氨基] -3-(甲氧基甲基)的治疗上有用的纯的,极性更大的非对映异构体的制备方法)-3-kefem-4-羧酸-1-(异丙氧基羰氧基)乙酯

摘要

Enterally absorbable diastereomers of (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(m ethoxymethyl)-3-cephem-4-carboxylic acid 1-(isopropoxycarbonyloxy)ethyl ester of the formula I IMAGE and its physiologically acceptable salts and also diastereomerically pure salts of the compounds of the general formula II IMAGE where HX represents a mono- or polybasic acid and where X represents an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II are described, which is characterised in that on mixing together one equivalent of a solution of the diastereomer mixture of the formula III with 0.2 - 2 equivalents of a solution of the acid component HY the more poorly soluble diastereomer of the general formula IV is first precipitated and separated off by filtration, then the more readily soluble diastereomer of the general formula IV is precipitated from the filtration solution, it being possible in the subsequent subsidiary steps for the acid components HY to be identical or different and any desired sequence of the addition of different acid components HY to be used, and the salts obtained are optionally further purified by crystallisation.
机译:(6R,7R)-7- [2-(2-氨基噻唑-4-基)-2-(Z)-(甲氧基亚氨基)乙酰胺基] -3-(间乙氧基甲基)-3-cephem-4-的肠溶性非对映异构体式I 的羧酸1-(异丙氧基羰基氧基)乙基酯及其生理上可接受的盐以及通式II 的化合物的非对映异构纯盐,其中HX表示一元或多元酸,而X表示描述了一种无机或有机生理上可接受的阴离子,以及制备这些式I或II化合物的方法,其特征在于将一当量的式III的非对映异构体混合物与0.2-的溶液混合在一起在2当量的酸组分HY的溶液中,首先沉淀出较难溶解的通式IV的非对映异构体,并通过过滤分离,然后从过滤溶液中沉淀出更易溶解的通式IV的非对映异构体,这是可能的。在随后的辅助步骤中,酸组分HY可以相同或不同,并且可以使用添加所需的不同酸组分HY的任何所需顺序,并且任选地通过结晶进一步纯化获得的盐。

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