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    • 10. 发明授权
    • Process for the preparation of oxazaphosphorine-2-amines
    • 制备恶唑烷-2-胺的方法
    • US06187941B1
    • 2001-02-13
    • US09149099
    • 1998-09-08
    • Ulf NiemeyerHarald NiegelBernard KutscherIon Neda
    • Ulf NiemeyerHarald NiegelBernard KutscherIon Neda
    • C07F924
    • C07F9/65846
    • A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction scheme in which R1 is H, 2-bromoethyl, 2-chloroethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl; R2 is H or 2-chloroethyl; R3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; and R4 is H; or R1 and R2, and also R3 and R4, together with the linked N atom, form an aziridide ring, where R1, R2 and R3 are not simultaneously H, and R1 and R3 are not simultaneously 1-phenylethyl; and Y, which is optionally present, is hydrogen chloride or hydrogen bromide. The reaction is carried out in a single vessel with phosphoryl chloride and an auxiliary base as an acid-binding agent with minimization of the effect of water and without isolation of an intermediate compound.
    • R1为H,2-溴乙基,2-氯乙基,2-羟基乙基,2-甲氧基乙基或1-苯基乙基的反应路线所述式(I)的恶唑烷磷胺-2-胺的制备方法。 R2是H或2-氯乙基; R3是H,2-溴乙基,2-氯乙基或1-苯基乙基; R4为H; 或R 1和R 2以及R 3和R 4与连接的N原子一起形成氮丙啶环,其中R 1,R 2和R 3不同时为H,并且R 1和R 3不同时为1-苯基乙基; 任选存在的Y是氯化氢或溴化氢。 该反应在具有磷酰氯和辅助碱作为酸结合剂的单个容器中进行,最小化水的作用并且不分离中间体化合物。