Process for the preparation of Imiquimod
    59.
    发明申请
    Process for the preparation of Imiquimod 审中-公开
    咪喹莫特的制备方法

    公开(公告)号:US20060004202A1

    公开(公告)日:2006-01-05

    申请号:US11159129

    申请日:2005-06-23

    IPC分类号: C07D471/02

    CPC分类号: C07D471/04

    摘要: A process for the preparation of Imiquimod and novel hydroxylamino and hydrazine derivatives, useful as intermediates in its preparation. The process includes the reaction of 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline, of formula (I) with a compound of formula (II) NH2—X  (II) wherein X is an —OR or —NR1R2 group, in which R is hydrogen, a C1-C6 alkyl, aryl-C1-C4 alkyl, aryl or —SO3H (sulfonic) group; and each of R1 and R2 is independently hydrogen, a C1-C6 alkyl, aryl-C1-C4 alkyl, aryl or —SO2R3 group, in which R3 is an aryl group and, if necessary, the reaction with a reducing agent.

    摘要翻译: 一种制备咪喹莫特和新型羟基氨基和肼衍生物的方法,可用作其制备中的中间体。 该方法包括式(I)的4-氯-1-异丁基-1H-咪唑并[4,5-c]喹啉与式(II)化合物的反应<?在线式描述=“In 线式公式“end =”lead“→NH 2 -X(II)<?in-line-formula description =”In-line Formulas“end =”tail“?>其中X是 -OR或-NR 1 R 2 R 2基,其中R是氢,C 1 -C 6亚基 烷基,芳基-C 1 -C 4烷基,芳基或-SO 3 H(磺酸基); 并且R 1和R 2各自独立地是氢,C 1 -C 6 - 烷基,芳基 - C 1 -C 4烷基,芳基或-SO 2 R 3 R 3基团,其中R 1,R 2,R 3, 3是芳基,如果需要,与还原剂反应。