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    7-amino-3-(pyrrolinium)methyl-3-cephem derivative
    92.
    发明专利
    7-amino-3-(pyrrolinium)methyl-3-cephem derivative 失效
    7-氨基-3-（吡咯烷）甲基-3-苯酚衍生物

    公开(公告)号：JPS6165886A

    公开(公告)日：1986-04-04

    申请号：JP18625784

    申请日：1984-09-07

    Applicant: Eisai Co Ltd

    Inventor： YAMAUCHI HIROSHI ,  SUGIYAMA ISAO ,  SAITO ISAO ,  NOMOTO SEIICHIRO ,  KAMIYA TAKU ,  MACHIDA YOSHIMASA ,  NEGI SHIGETO

    IPC: C07D501/18

    CPC classification number: Y02P20/55

    Abstract: NEW MATERIAL:A compound of formula I [n is 0, 1; R
    1 is H, protecting group; R
    2 is lower hydrocarbon; X is anion; when R
    3 is -COO
    - , m is 0, while m is 1, when R
    3 is -COOR
    4 (R
    4 is H, protecting group)] and its salt.
    EXAMPLE: 7β-Amino-3-(1-methyl-3-pyrrolinium)methyl-3-cephem-4-carboxylate.
    USE: An intermediate of antibacterials.
    PREPARATION: The reaction of a compound of formula II or its salt with another compound of formula III or its salt is carried out in an inert solvent such as acetone, THF or DMF at -10W50°C, when needed, deprotected and the reduction of sulfoxide is effected.
    COPYRIGHT: (C)1986,JPO&Japio

    Abstract translation: 新材料：式I化合物[n为0，1; R1为H，保护基; R2是低级烃; X是阴离子; 当R3为-COO - 时，m为0，而当m为1时，当R3为-COOR4时（R4为H，保护基）]及其盐。 实施例：7beta-氨基-3-（1-甲基-3-吡咯啉鎓）甲基-3-头孢烯-4-甲酸甲酯。 用途：抗菌药物的中间体。 制备：式Ⅱ化合物或其盐与另一种式Ⅲ化合物或其盐的反应在惰性溶剂如丙酮，THF或DMF中于-10-50℃进行，需要时脱保护， 亚砜的还原实现。

    SUBSTITUTED METHYLTHIOMETHYLCEPHALOSPORIN
    96.
    发明专利
    SUBSTITUTED METHYLTHIOMETHYLCEPHALOSPORIN 失效

    公开(公告)号：JPS60130590A

    公开(公告)日：1985-07-12

    申请号：JP23749483

    申请日：1983-12-15

    Applicant: SHIONOGI SEIYAKU KK

    Inventor： TSUJI SHIYOUJI ,  SATOU HISAO

    IPC: C07D501/18 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/57

    Abstract: NEW MATERIAL:7beta-Acylamino-3-(difluoromethyl or cyanomethyl)thiomethyl-3- cephem-4-carboxylic acid derivative of formula I (R is H, acyl; R is H, methoxy; R is difluoromethyl, cyanomethyl; R is H, lower metal, carboxyl-protecting group; X is -S-, -SO-). USE:Antibacterial against gram-positive and -negative bacteria. It has less side-effects. PREPARATION:The reaction of an amine of formula II or its reactive derivative with a carboxylic acid of ROH or its reactive derivative gives the objective compound.

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