Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid
monoamide derivatives
    7.
    发明授权
    Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives 失效
    2(R) - 苄基琥珀酸单酰胺衍生物的对映选择性合成方法

    公开(公告)号:US5321139A

    公开(公告)日:1994-06-14

    申请号:US22887

    申请日:1993-02-16

    摘要: Two processes are described for the preparation of the optically pure compounds of formula 1: ##STR1## in which R.sup.1 and R.sup.2 are e.g. alkyl, R.sup.3 and R.sup.4 are e.g. hydrogen and R.sup.5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C.dbd.C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.

    摘要翻译: 描述了制备光学纯的式1化合物的两种方法:其中R 1和R 2是例如: 烷基,R 3和R 4是例如。 氢和R 5是例如。 氢。 作为关键步骤,两种方法都包括C = C双键的对映选择性氢化和二羧酸单酰胺衍生物的区域选择性形成。 在一个过程中,苯基衣康酸衍生物被不对称氢化,得到光学活性(R) - 苄基琥珀酸,然后将其转化为二酯,所述二酯转化成式1的单酰胺化合物。在第二种方法中,苯基衣康酸衍生物 转化成其酐,然后将酸酐转化为单酰胺,然后将其不对称氢化,得到式1的化合物。