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    PROCESS FOR THE PRODUCTION OF AROMATIC AMINDES IN THE PRESENCE OF A PALLADIUM COMPLEX COMPRISING A FERROCENYL BIPHOSPHINE LIGAND
    1.
    发明申请
    PROCESS FOR THE PRODUCTION OF AROMATIC AMINDES IN THE PRESENCE OF A PALLADIUM COMPLEX COMPRISING A FERROCENYL BIPHOSPHINE LIGAND 审中-公开
    在含有呋喃核糖二磷酸盐配子的铂络合物存在下生产芳族氨基酸的方法

    公开(公告)号：US20100256417A1

    公开(公告)日：2010-10-07

    申请号：US12376583

    申请日：2007-08-06

    申请人： Harald Walter ,  Ulrike Nettekoven

    发明人： Harald Walter ,  Ulrike Nettekoven

    IPC分类号： C07C209/10

    CPC分类号： C07C209/10 ,  C07C2601/02 ,  C07C2603/66 ,  C07C211/61 ,  C07C211/45

    摘要： The present invention relates to a process for the preparation of compounds of Formula (I), wherein R1 is 1,3-dimethyl-butyl, 1,3,3-trimethyl-butyl or a group A1, wherein R3, R4 and R5 are each independently of the others hydrogen or C1-C4alkyl; and R2 is hydrogen; or R1 and R2 together from the group A2, wherein R6, and R7 are each independently of the other hydrogen or C1-C4alkyl; or R1 and R2 together from the group A3, wherein R5 and R9 are each independently of the other hydrogen or C1-C4alkyl; wherein a compound of Formula (II) wherein R1 and R2 are as defined for formula I and X is bromine or chlorine, is reacted with ammonia in the presence of a base and a catalytic amount of at least one palladium complex compound, wherein the palladium complex compound comprises at least one ferrocenyl-biphosphine ligand.

    摘要翻译： 本发明涉及一种制备式（I）化合物的方法，其中R 1是1,3-二甲基 - 丁基，1,3,3-三甲基 - 丁基或基团A1，其中R 3，R 4和R 5是 各自独立地为氢或C 1 -C 4烷基; R2是氢; 或R 1和R 2一起来自基团A2，其中R 6和R 7各自独立地为氢或C 1 -C 4烷基; 或R 1和R 2一起来自基团A3，其中R 5和R 9各自独立地为氢或C 1 -C 4烷基; 其中R 1和R 2如式I所定义，X为溴或氯的式（II）化合物在碱和催化量的至少一种钯络合物存在下与氨反应，其中钯 络合物包含至少一种二茂铁基 - 二膦配体。

    PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF
    3.
    发明申请
    PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF 审中-公开
    制备EZETIMIBE和中间体化合物的方法可用于制备它们

    公开(公告)号：US20100168414A1

    公开(公告)日：2010-07-01

    申请号：US12295442

    申请日：2007-09-29

    申请人： Ana Gavalda Escude ,  Jordi Bosch i Llado ,  Ulrike Nettekoven

    发明人： Ana Gavalda Escude ,  Jordi Bosch i Llado ,  Ulrike Nettekoven

    IPC分类号： C07D205/08

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.

    摘要翻译： 本发明一般涉及将式II化合物（下文）转化成式III化合物（下文）的改进方法，其是用于合成依泽替米贝或依泽替米贝本身的关键中间体，其中在式II和III中 ，R表示氢，烷基或羟基保护基（例如苄基，取代的苄基或甲硅烷基）。 本发明还包括所述方法的使用以及通过所述方法制备的式III化合物用于制备依泽替米贝的用途。