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1. 发明授权

US5441940A Process for the preparation of water soluble primycin and its components and pharmaceutical compositions containing them 失效
标题翻译：制备水溶性伯霉素及其组分和含有它们的药物组合物的方法
公开(公告)号：US5441940A
公开(公告)日：1995-08-15
申请号：US133795
申请日：1993-10-08
申请人： Tamas Keresztes , Andras Kover , Gabor Kulcsar , Katalin Erdodine , Gergelyne P. Katalin
发明人： Tamas Keresztes , Andras Kover , Gabor Kulcsar , Katalin Erdodine , Gergelyne P. Katalin
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C07H15/04
CPC分类号： C07H17/08
摘要： The invention relates to a process for the preparation of water soluble primycin and to the separation of its components of formulae (A.sub.1) and (A.sub.3) either as single components or as a mixture of the two components. According to the invention(i) water insoluble primycin is reacted in a C.sub.1-3 alcohol with a condensable substance comprising a C--C--C bridge in the presence of sodium or potassium methoxide or ethoxide, the resulting product with a water solubility of 40-60 mg/ml is separated, and, if desired,(ii) the resulting substance is subjected to column chromatography on silica gel applying a 1% aqueous solution of Partridge mixture as eluting agent to obtain a mixture of components of formulae (A.sub.1) and (A.sub.3) with a water solubility of 50 mg/ml, and, if desired,(iii) the resulting two-component mixture is subjected to ion exchange chromatography applying carboxymethyl cellulose in ammonium cycle as adsorbent and eluting the adsorbent with aqueous ammonium hydrocarbonate solution to obtain the component of formula (A.sub.3) with a water solubility of 50 mg/ml in pure form, and, if desired,(iv) elution is continued with absolute methanol comprising 10 mmoles of acetic acid to obtain the component of formula (A.sub.1) with a water solubility of 10 mg/ml in pure form.
摘要翻译：本发明涉及一种用于制备水溶性伯霉素的方法，以及将其式（A1）和（A3）的组分分离为单一组分或作为两种组分的混合物。根据本发明（i）水溶性伯霉素在甲醇钠或乙醇钠或甲醇钾存在下，在C 1-3醇与包含CCC桥的可冷凝物质反应，所得产物的水溶解度为40-60mg / ml，并且如果需要，（ii）将得到的物质在硅胶上进行柱色谱，用1％的鹧鸪混合物水溶液作为洗脱剂，得到式（A1）和（A3）的组分的混合物，水溶解度为50mg / ml，如果需要，（iii）将得到的双组分混合物进行离子交换色谱，在铵循环中用羧甲基纤维素作为吸附剂，并用碳酸氢铵水溶液洗脱该吸附剂，得到水溶性为纯净形式为50mg / ml的式（A3）组分，如果需要，（iv）用包含10mmol乙酸的无水甲醇继续洗脱，得到f （A1），水溶性为10mg / ml，纯净。

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