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    • 9. 发明专利
    • Fluoromethylthiooxacephalosporin
    • FLUOROMETHYLTHIOOXACEPHALOSPORIN
    • JPS59139385A
    • 1984-08-10
    • JP23447282
    • 1982-12-23
    • Shionogi & Co Ltd
    • TSUJI SHIYOUJISATOU HISAOHAMASHIMA YOSHIO
    • C07D498/04A61K31/535A61P31/04C07D505/00
    • C07D505/00Y02P20/55
    • NEW MATERIAL:A 7β-(fluorinated methylthioacetamido)-7α-methoxy-3-(1-hydroxyalkyl-5-tetrazolyl)thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid shown by the formula I [R is FCH
      2 -, F
      2 CH-; R
      1 is R
      3 O-substituted alkyl (R
      3 is H, or OH-protecting group); R
      2 is H, light metal, or carboxyl group], or a derivative at its carboxyl or hydroxalkyl group.
      EXAMPLE: 7β-[Difluoromethylthioacetamido-7α-methoxy-3-( 1-benzyloxycarbonyloxyethyl-5-tetrazolyl )thiomethyl]-1-dethia-1-oxa-3-cephem-4-carboxylic acid diphenylmethyl ester.
      USE: An antibacterial agent.
      PROCESS: An amine(reactive derivative) shown by the formula II is reacted with a methylthioacetic acid fluoride (reactive derivative) shown by the formula RSCH
      2 COOH.
      COPYRIGHT: (C)1984,JPO&Japio
    • 新材料:式I所示的7a-(氟化甲硫基乙酰氨基)-7α-甲氧基-3-(1-羟基烷基-5-四唑基)甲基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸 [R是FCH 2 - ,F 2 CH-; R 1是R 3 O-取代的烷基(R 3是H或OH保护基); R 2是H,轻金属或羧基]或其羧基或羟烷基上的衍生物。 实施例:7beta- [二氟甲硫基乙酰氨基-7α-甲氧基-3-(1-苄氧羰基氧基乙基-5-四唑基)硫甲基] -1-脱硫-1-氧杂-3-头孢烯-4-羧酸二苯基甲酯。 用途:抗菌剂。 方法:由式II所示的胺(反应性衍生物)与式RSCH 2 COOH所示的甲硫基乙酸氟化物(反应性衍生物)反应。