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    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates
    21.
    发明授权
    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates 失效
    氟化甲基氨基链烷酸的制备和新工艺中间体

    公开(公告)号：US4353828A

    公开(公告)日：1982-10-12

    申请号：US170395

    申请日：1980-07-21

    申请人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    发明人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    IPC分类号： C07F3/02 ,  C07C87/26 ,  C07D209/48

    CPC分类号： C07F3/02 ,  Y02P20/55

    摘要： Fluorinated alkenylamines of the Formula V ##STR1## wherein n represents 0, 1, 2 or 3; R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl and Y represents (a), when n represents O, CH.sub.2 F, (b), when n represents 1, CH.sub.2 F or CHF.sub.2, or (c) when n represents 2 or 3, CH.sub.2 F, CHF.sub.2 or CF.sub.3 are novel process intermediates. They are obtained by hydrolysis and subsequent reduction of the corresponding alkenyl fluorinated methyl ketimine magnesium halides, which are novel compounds resulting from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized while the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmacological or anti-bacterial agents.

    摘要翻译： 式V的氟化烯基胺其中n表示0,1,2或3; R1表示氢或C1-C10烷基，Y表示（a），当n表示O，CH2F，（b）时，当n表示1时，CH2F或CHF2，或（c）当n表示2或3时，CH2F，CHF2或 CF3是新型工艺中间体。 它们通过水解和随后还原相应的烯基氟代甲基酮亚胺卤化镁得到，其是由相应的烯基卤化镁与相应的氟化乙腈反应得到的新化合物。 式V的氟化链烯基胺被氧化，同时保护氨基以除去胺保护基之后提供相应的氟化甲基氨基链烷酸，其是有用的药理学或抗菌剂。