Dextro 1-methyl-2-(2-naphthyl) aziridine
    1.
    发明授权
    Dextro 1-methyl-2-(2-naphthyl) aziridine 失效
    右旋1-甲基-2-(2-萘基)氮丙啶

    公开(公告)号:US3890302A

    公开(公告)日:1975-06-17

    申请号:US25983972

    申请日:1972-06-05

    CPC classification number: C07D203/08

    Abstract: Racemic 1-methyl-2-(2-naphthyl)aziridine, being useful as a tranquilizer, is prepared via three routes: (a) halogenation of the corresponding aminoalcohol and treatment of the resulting haloamine with an alkali; (b) treatment of the corresponding aminoalcohol with sulfuric acid and treatment of the resulting hydrogen sulfate with an alkali; and (c) treatment of 2-(2naphthyl)aziridine with an oxonium methylating agent. Dextro-1methyl-2-(2-naphthyl)aziridine, being more potent in the tranquilizing activity than the racemate, is prepared by optical resolution of racemic 2-(2-naphthyl)-2-methylaminoethanol with levo-tartaric acid, treatment of the resulting dextro-2-(2naphthyl)-2-methylaminoethanol levo-tartrate with an alkali, treatment of the resulting dextro-2-(2-naphthyl)-2methylaminoethanol with a halogenating agent and treatment of the resulting levo-N-methyl-2-halogeno-1-(2-naphthyl)ethylamine with an alkali.

    Abstract translation: 通过三种途径制备用作镇定剂的外消旋1-甲基-2-(2-萘基)氮丙啶:(a)卤化相应的氨基醇并用碱处理得到的卤代胺; (b)用硫酸处理相应的氨基醇,用碱处理得到的硫酸氢盐; 和(c)用氧代甲基化剂处理2-(2-萘基)氮丙啶。 通过用左旋酒石酸旋光拆分外消旋的2-(2-萘基)-2-甲基氨基乙醇,制备了比外消旋物更有效的镇痛活性的右旋-1-甲基-2-(2-萘基)氮丙啶, 用碱处理得到的右旋-2-(2-萘基)-2-甲基氨基乙醇左旋酒石酸盐,用卤化剂处理所得的右旋-2-(2-萘基)-2-甲基氨基乙醇,并处理所得的 左旋-N-甲基-2-卤代-1-(2-萘基)乙胺与碱反应。

    Improved process for preparing n-benzylically substituted aziridines
    2.
    发明授权
    Improved process for preparing n-benzylically substituted aziridines 失效
    制备N-叔丁基取代的亚胺酯的改进方法

    公开(公告)号:US3855217A

    公开(公告)日:1974-12-17

    申请号:US24687372

    申请日:1972-04-24

    Inventor: THILL B

    CPC classification number: C07D203/08

    Abstract: N-Benzylically substituted aziridines are conventionally prepared by reacting a benzyl halide with aziridine (or other non-N-substituted aziridine) in the presence of an acid acceptor. Product yields are considerably improved by conducting the above process in a liquid aromatic hydrocarbon reaction medium. E.g., N-benzylaziridine is prepared in excellent yields by reacting benzyl chloride with aziridine in the presence of powdered KOH and benzene.

    Abstract translation: N-苄基取代的氮丙啶通常在酸受体存在下使苄基卤与氮丙啶(或其它非N-取代的氮丙啶)反应制备。 通过在液体芳族烃反应介质中进行上述方法,产物产率显着提高。 例如,通过苄基氯与氮丙啶在粉末状KOH​​和苯的存在下反应制得N-苄基氮丙啶。

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