CRYSTALLINE FORM II OF 7-(DIMETHOXY-METHYL) CAMPTOTHECIN, ITS USE AS INTERMEDIATE AND PRODUCTS OBTAINED THEREFROM
    4.
    发明申请
    CRYSTALLINE FORM II OF 7-(DIMETHOXY-METHYL) CAMPTOTHECIN, ITS USE AS INTERMEDIATE AND PRODUCTS OBTAINED THEREFROM 有权
    7-(二甲氧基甲基)氨基甲酸酯的晶体形式II,作为中间体使用,并由其获得的产物

    公开(公告)号:US20100249414A1

    公开(公告)日:2010-09-30

    申请号:US12670905

    申请日:2008-07-22

    IPC分类号: C07D471/20

    CPC分类号: C07D491/22

    摘要: This invention relates to a process for preparing a crystalline form of (4S)-11-(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]qui-noline-3,14(4H,12H)-dione (also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing it from methanol.

    摘要翻译: 本发明涉及制备(4S)-11-(二甲氧基甲基)-4-乙基-4-羟基-1H-吡喃并[3',4':6,7]吲哚并[1,2- b]喹啉-3,14(4H,12H) - 二酮(也称为7-(二甲氧基 - 甲基)喜树碱)。 通过提供特定的结晶步骤,以合适的方式得到上述化合物的新结晶形式。 制备多晶型II的方法包括将喜树碱转化成相应的7-(二甲氧基 - 甲基)喜树碱,并将其从甲醇中结晶。