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    Process for the preparation of chemical compounds
    3.
    发明授权
    Process for the preparation of chemical compounds 失效
    化合物的制备方法

    公开(公告)号：US06756498B2

    公开(公告)日：2004-06-29

    申请号：US10258679

    申请日：2002-10-25

    申请人： Russ N. Fitzgerald ,  David Kendall Jung ,  John F Eaddy

    发明人： Russ N. Fitzgerald ,  David Kendall Jung ,  John F Eaddy

    IPC分类号： C07D47104

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulfonyl, C1-6alkoxy substituted by one or more fluorine atoms, halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R6, or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R6 is halogen, C1-6alkyl, C1-6alkoxy or C1-6alkoxy substituted by one or more fluorine atoms; which comprises rearrangement of an azirine of formula (II)  wherein R0 to R3 are as defined for formula (I), or a protected derivative thereof, in the presence of a catalyst and a solvent.

    摘要翻译： 本发明提供了制备式（I）化合物及其药学上可接受的衍生物的方法，其中：R 0和R 1独立地选自H，卤素，C 1-6烷基，C 1-6烷氧基或C 1-6烷氧基 被一个或多个氟原子取代; R 2是H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（ O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，卤素，CN，CONR 4 R 5，CO 2 H，CO 2 C 1-6烷基或NHSO 2 R 4; R 3， 是H或被SO 2 C 1-6烷基或SO 2 NH 2取代的苯基; R 4和R 5独立地选自H，C 1-6烷基，苯基，被一个或多个原子或基团R 6取代的苯基，或与 它们所连接的氮原子形成饱和的4至8元环R 6是卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基;其包括将式 II）其中R 0至R 3为 如式（I）所定义，或其保护的衍生物在催化剂和溶剂的存在下反应。