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    Preparation of 1H-imidazo[4,5-C] quinolin 4-amines via novel 1H-imidazo[4,5-c] quinolin 4-cyano and 1H-imidazo[4,5-c] quinolin 4-carboxamide intermediates
    10.
    发明授权
    Preparation of 1H-imidazo[4,5-C] quinolin 4-amines via novel 1H-imidazo[4,5-c] quinolin 4-cyano and 1H-imidazo[4,5-c] quinolin 4-carboxamide intermediates 失效
    通过新的1H-咪唑并[4,5-c]喹啉4-氰基和1H-咪唑并[4,5-c]喹啉-4-甲酰胺中间体制备1H-咪唑并[4,5-C]喹啉-4-胺

    公开(公告)号：US07166721B2

    公开(公告)日：2007-01-23

    申请号：US11009259

    申请日：2004-12-09

    申请人： Valeriano Merli ,  Silvia Mantovani ,  Stefano Bianchi

    发明人： Valeriano Merli ,  Silvia Mantovani ,  Stefano Bianchi

    IPC分类号： C07D471/06 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c]quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.

    摘要翻译： 本发明涉及合成1H-咪唑并[4,5-c]喹啉4-氰基和1H-咪唑并[4,5-c]喹啉4-甲酰胺中间体的方法，可用于制备1H-咪唑并[4,5 -C]喹啉-4-胺，使用这种中间体制备1H-咪唑并[4,5-C]喹啉-4-胺的方法; 和1H-咪唑并[4,5-c]喹啉4-氰基和1H-咪唑并[4,5-c]喹啉4-甲酰胺中间体。 更具体地说，本发明涉及使用两个中间体1-异丁基-1H-咪唑并[4,5-噻唑并[4,5-c]喹啉-4-胺（咪喹莫德）制备1-异丁基-1H-咪唑并[4,5-C] c]喹啉4-氰基和1-异丁基-1H-咪唑并[4,5-c]喹啉4-甲酰胺，并且与所述中间体反应。