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    • 3. 发明申请
    • PROCESS FOR PURIFICATION OF MACROLIDES
    • MACROLIDES净化工艺
    • WO2008059516A2
    • 2008-05-22
    • PCT/IN2007/000352
    • 2007-08-16
    • CONCORD BIOTECH LIMITEDNARULA, PardeepPATEL, JayeshVAID, SudhirPATEL, Pragnesh
    • NARULA, PardeepPATEL, JayeshVAID, SudhirPATEL, Pragnesh
    • A61K31/4745
    • C07D498/08
    • The invention is a novel process for purification of macrolides such as Tacrolimus using a new polymer resin and copper salts containing cupric ions. The novel polymer resin contains polyvinyl pyrrolidone, metha acrylate, divinyl benzene based compounds. In the said process manufacturing of new polymer resin and use of cupric salt is very much cost effective. The same metal salts can also be used along with other neutral non-ionic adsorption resins of polyethylene i e HP2O, HP2OSS, Sepabeads SP207 and the like. The concentration of copper ions may be generally 0.20 to 1.5 mol/L, preferably 0.30 to 0.40 mol/L. As an aqueous medium for the copper ion containing aqueous solvent, an aqueous acetone, an aqueous alcohol, an aqueous acetonitrile or the like. The invention covers Tacrolimus having a purity of more than 99.7%.
    • 本发明是使用新的聚合物树脂和含有铜离子的铜盐来纯化大环内酯如塔克罗莫司的新方法。 新型聚合物树脂含有聚乙烯吡咯烷酮,甲基丙烯酸酯,二乙烯基苯基化合物。 在所述方法中制造新型聚合物树脂和使用铜盐是非常成本有效的。 同样的金属盐也可以与聚乙烯的其它中性非离子吸附树脂一起使用,例如HP2O,HP2OSS,Sepabeads SP207等。 铜离子的浓度通常为0.20〜1.5mol / L,优选为0.30〜0.40mol / L。 作为含有铜离子的含水溶剂的水性介质,含水丙酮,含水醇,乙腈水溶液等。 本发明涵盖具有超过99.7%纯度的他克莫司。