Novel cephem compound and its preparation
    8.
    发明专利
    Novel cephem compound and its preparation 失效
    新型化合物及其制备

    公开(公告)号:JPS59116290A

    公开(公告)日:1984-07-05

    申请号:JP22021683

    申请日:1983-11-22

    CPC分类号: C07D501/22 C07D501/24

    摘要: NEW MATERIAL:The compound of formula I [R
    1 is amino or acylamino; R
    2 is 2,2-dihalovinyl or ethynyl; R
    3 is (protected) carboxy] and its salt.
    EXAMPLE: 7-[ 2-Methoxyimino-2-( 2-aminothiazol-4-yl )acetamide-3-( 2,2-dichlorovinyl)-3-cephem-4-carboxylic acid (syn isomer).
    USE: Preventive and remedy for microbism.
    PROCESS: The objective compound is prepared by reducing the compound of formula II or its salt with a reducing agent comprising a combination of e.g. stannous chloride and acetyl chloride, etc., usually under cooling or at room temperature.
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译: 新材料:式I化合物[R 1]是氨基或酰氨基; R2是2,2-二卤乙烯基或乙炔基; R 3是(保护的)羧基]及其盐。 实例:7-〔2-甲氧基亚氨基-2-(2-氨基噻唑-4-基)乙酰胺-3-(2,2-二氯乙烯基)-3-头孢烯-4-羧酸(顺式异构体)。 用途:微生物的预防和补救。 方法:目标化合物是通过用还原剂还原式II化合物或其盐来制备的,所述还原剂包括组合例如 氯化亚锡和乙酰氯等,通常在冷却或室温下。

    2-substituted cephem derivative and its preparation
    9.
    发明专利
    2-substituted cephem derivative and its preparation 失效
    2-取代的CEPHEM衍生物及其制备

    公开(公告)号:JPS5946292A

    公开(公告)日:1984-03-15

    申请号:JP15758182

    申请日:1982-09-09

    CPC分类号: C07D501/22 Y02P20/55

    摘要: NEW MATERIAL:The compound of formula I [R
    1 is (substituted) phenyl(methyl) or (substituted) phenoxymethyl; R
    2 is H or carboxylic acid-protecting group; Y is allyloxy, benzyloxy, alkylthio, group of formula IIWIV (R
    4 and R
    6 are H or lower alkyl; X is O, S, etc.; R
    5 is H, lower alkyl or phenyl), etc.].
    EXAMPLE: 2-Allyloxy-7-phenoxy-acetamido-3'-desacetoxycephalosporinic acid benzyl ester of formula V.
    USE: An intermediate for the synthesis of antibacterial agent.
    PROCESS: The cephem derivative of formula VI (R
    3 is lower alkyl or acyl) is made to react with the nucleophilic agent of formula Y-H in the presence of an acid or iodine.
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译: 新物质:式I化合物[R 1]为(取代的)苯基(甲基)或(取代的)苯氧基甲基; R 2是H或羧酸保护基; Y是烯丙氧基,苄氧基,烷硫基,式II-IV基(R 4和R 6)是H或低级烷基; X是O,S等; R 5是H,低级烷基或苯基 )等]。 实施例:式V的2-烯丙氧基-7-苯氧基 - 乙酰氨基-3'-去乙酸基头孢菌酸苄酯。用途:合成抗菌剂的中间体。 方法:使式VI的头孢烯衍生物(R 3是低级烷基或酰基)在酸或碘的存在下与式Y-H的亲核剂反应。