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    Process for the preparation of penam derivatives
    1.
    发明公开
    Process for the preparation of penam derivatives 失效
    一种制备Penamderivaten过程。

    公开(公告)号：EP0070103A1

    公开(公告)日：1983-01-19

    申请号：EP82303111.7

    申请日：1982-06-16

    申请人： BEECHAM GROUP PLC

    发明人： Dales, John Robert Mansfield ,  Vallance, Marguerita Anne

    IPC分类号： C07D499/04

    CPC分类号： C07D499/00

    摘要： A process for the preparation of a penam derivative of formula (I):
    wherein R A is hydrogen or a group of formula (la):
    wherein X is -C0 2 R', or S0 3 R'; R is C 1-6 alkyl, aryl, or heterocyclyl; R' is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R 2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolysable ester-forming radical; which process comprises reacting a compound of formula (II):
    wherein R B is hydrogen, a removable amino blocking group, or a group of formula (Ila):
    wherein Y is -CO 2 R x or -SO 3 R x ; R is as defined with respect to formula (I) above; R x represents an ester-forming radical, R y represents hydrogen, a salt-forming radical or a carboxyl-blocking group, and R 3 represents an alkyl, benzyl, or aryl group; with methanol in the presence of copper ions; and thereafter if necessary carrying out one or more of the following steps:

    (i) removal of any blocking group;
    (ii) converting the product to a pharmaceutically acceptable salt or ester thereof.

    Process for the preparation of hydroxyphenyl hydantoin and of hydroxyphenyl glycine, and compounds thus obtained
    2.
    发明公开
    Process for the preparation of hydroxyphenyl hydantoin and of hydroxyphenyl glycine, and compounds thus obtained 失效
    由此获得一种用于制备hydroxyphenylhydantoin和羟基苯基甘氨酸，和化合物的方法。

    公开(公告)号：EP0001319A1

    公开(公告)日：1979-04-04

    申请号：EP78300214.0

    申请日：1978-07-31

    申请人： BEECHAM GROUP PLC

    发明人： Dales, John Robert Mansfield

    IPC分类号： C07D233/78 ,  C07C101/72 ,  C12D13/06

    CPC分类号： C07D233/78

    摘要： 5-(a-Hydroxyphenyl) hydantoin of formula (I):
    is prepared by reacting phenol, glyoxylic acid and urea in the presence of an acid catalyst in an aqueous medium.
    The hydantoin may be hydrolysed to produce the amino acid,p-hydroxyphenylglycine, preferably to the D-amino acid, either by selective enzymatic hydrolysis and subsequent chemical hydrolysis, or by alkaline hydrolysis and subsequent resolution.

    摘要翻译： 式（I）的5-（对羟苯基）乙内酰脲：通过在给wässrige介质中反应的酚，乙醛酸和尿素在酸催化剂的存在下制备。 乙内酰脲可被水解，或通过碱的水解和随后的分辨率来产生的氨基酸，对 - 羟基苯基甘氨酸，优选为D-氨基酸，无论是通过选择性酶促水解和随后的化学水解。