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    METHOD FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND, SYNTHESIS INTERMEDIATES THEREOF AND METHODS FOR OBTAINING THEM
    9.
    发明申请
    METHOD FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND, SYNTHESIS INTERMEDIATES THEREOF AND METHODS FOR OBTAINING THEM 审中-公开
    获得药物活性化合物的方法，其合成中间体及其获得的方法

    公开(公告)号：WO2007003522A1

    公开(公告)日：2007-01-11

    申请号：PCT/EP2006/063534

    申请日：2006-06-26

    申请人： INKE, S.A. ,  PEREZ ANDRES, Juan Antonio ,  DALMASES BARJOAN, Pere

    发明人： PEREZ ANDRES, Juan Antonio ,  DALMASES BARJOAN, Pere

    IPC分类号： C07D451/14 ,  C07D471/18

    CPC分类号： C07D471/18 ,  C07D451/14

    摘要： The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.

    摘要翻译： 本发明涉及一种获得杜拉司琼的方法，该方法包括：a）式（Ⅳ）的醇与吲哚-3-羧酸（化合物（Ⅲ））或其活性衍生物酯化，得到式 V），然后是步骤b），其包括中间体（V）的Dieckmann反应，通过与强有机或无机碱反应，得到中间体（VI），和步骤c），其包括中间体（VI）的反式羟基羰基化反应， 给予多沙司琼碱，以及如果需要，其药学上可接受的盐，所述盐的碱的水合物或溶剂合物。 本发明还涉及中间体（V）和（VI）及其获得方法。 利用本发明的方法，以工业规模获得了具有良好产率的Dolasetron，反应物和溶剂的使用减少，而所述方法也具有更高的原子效率。