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    METHOD FOR PRODUCING 6-HYDROXYETHYLPENAM COMPOUND
    1.
    发明公开
    METHOD FOR PRODUCING 6-HYDROXYETHYLPENAM COMPOUND 有权
    生产6-羟基乙基苯胺化合物的方法

    公开(公告)号：EP2123657A1

    公开(公告)日：2009-11-25

    申请号：EP08721477.1

    申请日：2008-03-06

    申请人： OTSUKA CHEMICAL COMPANY, LTD.

    发明人： TANAKA, Hideo ,  KUROBOSHI, Manabu ,  TATEYAMA, Syoichi ,  YAMADA, Takae ,  KAMEYAMA, Yutaka

    IPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897

    CPC分类号： C07D499/04 ,  C07D499/861 ,  C07D499/897 ,  Y02P20/55

    摘要： The present invention provides a method by which a 6-hydroxyethyl penam compound represented by General Formula (2) below can be produced with a high selectivity:

    wherein R represents a hydrogen atom or a protective group for carboxylic acid and X 2 represents a halogen atom;
    the method including the steps of reacting a Grignard reagent with a halogeno penam compound represented by General Formula (1) below:

    wherein R and X 2 are the same as above, and X 1 represents a halogen atom;
    reacting the generated compound with an amine compound; and
    further reacting the generated compound with acetaldehyde.

    摘要翻译： 本发明提供了一种可以以高选择性制备下述通式（2）表示的6-羟乙基青霉素化合物的方法：其中R代表氢原子或羧酸保护基团，并且X 2代表卤素原子; 所述方法包括以下步骤：使格利雅试剂与由以下通式（1）表示的卤代青霉烷化合物反应：其中R和X2与上述相同，并且X1表示卤素原子; 使生成的化合物与胺化合物反应; 并进一步使生成的化合物与乙醛反应。

    Process for the preparation of penam derivatives
    4.
    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 preparing penicillin sulfoxides
    5.
    发明公开
    Process for preparing penicillin sulfoxides 失效
    Verfahren zur Herstellung von Penicillinsulfoxiden。

    公开(公告)号：EP0017419A1

    公开(公告)日：1980-10-15

    申请号：EP80300923.2

    申请日：1980-03-25

    申请人： ELI LILLY AND COMPANY

    发明人： Chou, Ta-Sen

    IPC分类号： C07D499/04 ,  C07D499/44 ,  C07D499/42

    CPC分类号： C07D499/00

    摘要： A 4-thia-1-azobicyclo (3.2.0) heptane nucleus bearing compound, e.g. a penicillin, is treated with a peroxymonosulfate at from about 0°C to about 50°C in an aqueous medium to form the compound having the corresponding 4-sulfoxide nucleus.

    摘要翻译： 具有4-硫杂-1-偶氮双环（3.2.0）庚烷核的化合物，例如 青霉素在约0℃至约50℃的过氧化硫酸盐水溶液中处理以形成具有相应的4-亚砜核的化合物。