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    PHARMACEUTICAL INTERMEDIATES IN THE SYNTHESIS OF ACE-INHIBITORS AND THE USE THEREOF
    26.
    发明申请
    PHARMACEUTICAL INTERMEDIATES IN THE SYNTHESIS OF ACE-INHIBITORS AND THE USE THEREOF 有权
    ACE抑制剂合成中的药物中间体及其用途

    公开(公告)号：US20100286404A1

    公开(公告)日：2010-11-11

    申请号：US12300545

    申请日：2007-05-11

    申请人： Marta Porcs-Makkay ,  Gyula Simig ,  Tibor Mezei ,  Angéla Veressné Pandur ,  Gyula Lukács

    发明人： Marta Porcs-Makkay ,  Gyula Simig ,  Tibor Mezei ,  Angéla Veressné Pandur ,  Gyula Lukács

    IPC分类号： C07D263/44 ,  C07D209/52 ,  C07D209/42 ,  C07C69/96

    CPC分类号： C07K5/0222 ,  A61K38/00 ,  C07C271/22 ,  C07D209/42 ,  C07D263/44

    摘要： The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

    摘要翻译： 通式（I）的化合物，其中R 1是芳基或烷基; R2代表烷基; R3表示烷基或芳烷基，是有价值的药物中间体，其可以通过使通式（IV）化合物（其中R 1和R 2的定义如上所述）与至少2摩尔当量的 通式（VI）（其中X表示卤素或叔丁氧羰基氧基，R3如上定义）。 通式（II）的已知化合物（其中R1和R2如上定义）通过使通式（I）的化合物与亚硫酰氯反应来制备。 通式（I）的化合物是可用于合成药物活性成分的新中间体，特别是在制备ACE抑制剂中。 依那普利，培哚普利或雷米普利。