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    • 10. 发明授权
    • Method for preparing atosiban acetate
    • 阿托品醋酸酯的制备方法
    • US09434767B2
    • 2016-09-06
    • US13579030
    • 2011-12-22
    • Qing XiaoJian LiuHongling LiYaping MaJiancheng Yuan
    • Qing XiaoJian LiuHongling LiYaping MaJiancheng Yuan
    • C07K7/64C07K7/16
    • C07K7/64C07K7/16
    • The present invention provides a method for preparing atosiban acetate. The method comprises the following steps of: synthesizing to obtain linear atosiban; dissolving the linear atosiban in an acetonitrile aqueous solution, adjusting the pH value with ammonia water, adding H2O2 for oxidizing, filtering, purifying, and transferring salt to obtain the atosiban acetate. In the present invention, an appropriate route is provided, the linear atosiban is synthesized by adopting a solid phase method, and the atosiban is obtained by liquid phase oxidation. The method has the advantages of capabilities of solving the problem of insolubility of the linear atosiban, reducing the reaction size to the maximum extent and shortening reaction time, and being high in yield and easy to industrialize.
    • 本发明提供了一种制备醋酸托西班醋酸酯的方法。 该方法包括以下步骤:合成得到线性阿托西班; 将线性阿托西班溶解在乙腈水溶液中,用氨水调节pH值,加入H 2 O 2进行氧化,过滤,纯化和转移盐,得到醋酸阿托品。 在本发明中,提供了适当的途径,通过采用固相法合成线性阿托西班,通过液相氧化获得阿托西班。 该方法具有解决线性阿托西班不溶性问题的能力,最大限度地减少反应尺寸,缩短反应时间,产率高,易于工业化的优点。