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    SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF PRAMIPEXOL
    2.
    发明申请
    SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF PRAMIPEXOL 失效
    合成制备PRAMIPEXOL的中间体

    公开(公告)号：US20070166814A1

    公开(公告)日：2007-07-19

    申请号：US11622259

    申请日：2007-01-11

    申请人： Sergio RIVA ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Sergio RIVA ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C12P41/00

    CPC分类号： C12P17/14 ,  C07D277/82 ,  C12P41/005

    摘要： A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R, S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.

    摘要翻译： 制备式（I）的酸作为单个（R）对映异构体或（S）的方法或其盐，其中R是被保护的氨基; 并且星号*表示立体碳原子，包括使式（II）的酯作为（R，S）对映体或其盐的混合物，其中R 1是直链或支链C 任选被苯基取代的C 1 -C 6烷基; 在有效获得包含式（I）的酸的混合物作为单独的（R）对映异构体和式（II）的酯的混合物的条件下，将来自南极念珠菌的脂肪酶与式（II）的酯作为 个体（S）对映体; 随后水解后者以获得式（I）的酸作为单独的（S）对映异构体; 如果需要，将式（I）的酸作为（R）或（S）对映异构体转化为其盐。

    Synthesis of intermediates for the preparation of pramipexol
    3.
    发明授权
    Synthesis of intermediates for the preparation of pramipexol 失效
    用于制备普拉克索的中间体的合成

    公开(公告)号：US07662610B2

    公开(公告)日：2010-02-16

    申请号：US11622259

    申请日：2007-01-11

    申请人： Sergio Riva ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Sergio Riva ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C12P41/00

    CPC分类号： C12P17/14 ,  C07D277/82 ,  C12P41/005

    摘要： A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; (the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.

    摘要翻译： 制备式（I）的酸作为单个（R）对映异构体或（S）的方法或其盐，其中R是被保护的氨基; 并且星号*表示立体碳原子，包括使式（II）的酯作为（R，S）对映体或其盐的混合物接触，其中R 1是直链或支链的C 1 -C 6烷基，任选被苯基 ; （上文定义的星号*和R）与来自南极念珠菌的脂肪酶在有效获得包含式（I）的酸的混合物作为个体（R）对映异构体的条件下，和式（II）的酯， 作为个体（S）对映体; 随后水解后者以获得式（I）的酸作为单独的（S）对映异构体; 如果需要，将式（I）的酸作为（R）或（S）对映异构体转化为其盐。