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    PREPARATION METHOD OF FOSAMPRENAVIR DERIVATIVES AND RELEVANT INTERMEDIATE THEREOF
    2.
    发明公开
    PREPARATION METHOD OF FOSAMPRENAVIR DERIVATIVES AND RELEVANT INTERMEDIATE THEREOF 审中-公开
    ZERISHEN ZUR HENTELLUNG VON FOSAMPRENAVIR-DERIVATEN UND ZWISCHENPRODUKTEN DAVON

    公开(公告)号：EP2634192A1

    公开(公告)日：2013-09-04

    申请号：EP11835623.7

    申请日：2011-10-26

    申请人： Zhejiang Jiuzhou Pharma Science & Technology Co., Ltd.

    发明人： XU, Jiankang ,  YE, Meiqi ,  CHEN, Bin ,  XU, Qiaoqiao

    IPC分类号： C07F9/655

    CPC分类号： C07F9/65515

    摘要： Preparation method of fosamprenavir derivatives is disclosed. The compound shown by formula II or its ammonium salt is reacted with a metal ion source in solvent to obtain the compound shown by formula III. After isolating and purifying, the compound shown by formula III is catalytically reduced to the compound shown by formula I. In the formula, X is metal ion. Preferably, the metal ion source is a calcium ion source, sodium ion source, or potassium ion source, and X is calcium ion, sodium ion, or potassium ion. The solvent is methanol, ethanol, n-propanol, iso-propanol, n-butanol, or sec-butanol. The catalytic reduction is carried out by using hydrogen as a reducing agent in the presence of palladium on carbon catalyst. The ammonium salt is methylamine salt, dimethylamine salt, ethylamine salt, diethylamine salt, isopropylamine salt, dibutylamine salt, dipropylamine salt, t-butylamine salt, or dicyclohexylamine salt. The relevant intermediate of fosamprenavir derivatives in the preparation method is also provided. The preparation method of fosamprenavir derivatives reduces the cost, improves the productivity, and is applicable for large-scale popularization and application.

    摘要翻译： 披露了福沙那韦衍生物的制备方法。 将式II化合物或其铵盐与溶剂中的金属离子源反应，得到式III所示的化合物。 分离纯化后，将式III化合物催化还原成式I所示的化合物。在该式中，X为金属离子。 优选地，金属离子源是钙离子源，钠离子源或钾离子源，X是钙离子，钠离子或钾离子。 溶剂是甲醇，乙醇，正丙醇，异丙醇，正丁醇或仲丁醇。 催化还原通过在钯/碳催化剂存在下使用氢作为还原剂进行。 铵盐是甲胺盐，二甲胺盐，乙胺盐，二乙胺盐，异丙胺盐，二丁胺盐，二丙胺盐，叔丁胺盐或二环己胺盐。 还提供了制备方法中福沙那韦衍生物的相关中间体。 福沙那韦衍生物的制备方法降低成本，提高生产率，适用于大规模普及应用。