Process for the synthesis of 3-cyano-6-alkoxy-7-nitro-4-quinolones
    1.
    发明授权
    Process for the synthesis of 3-cyano-6-alkoxy-7-nitro-4-quinolones 失效
    合成3-氰基-6-烷氧基-7-硝基-4-喹诺酮的方法

    公开(公告)号:US06933388B2

    公开(公告)日:2005-08-23

    申请号:US10820115

    申请日:2004-04-07

    IPC分类号: C07D215/56 C07D215/36

    CPC分类号: C07D215/56

    摘要: There is provided a process for the preparation of 3-cyano-6-alkoxy-7-nitro-4-quinolone intermediates useful for the preparation of protein tyrosine kinase (PTK) inhibitors which are useful in the treatment of cancer of the formula: wherein R is alkyl(C1-C3) prepared by reacting a substituted anthranilate with N,N-dimethylformamide dimethyacetal to obtain a N,N-dimethylamidine which is condensed with t-butylcyanoacetate to obtain a N-(2-cyano-2-t-butoxycarbonylvinyl)anthranilate, which is hydrolyzed to yield a N-(2-cyano-2-carboxyvinyl)anthranilate followed by decarboxylating to obtain a N-(2-cyano-2-carboxyvinyl)anthranilate followed by cyclizing to obtain a 3-cyano-6-alkoxy-7-nitro-4-quinolone.

    摘要翻译: 提供了用于制备可用于治疗下列癌症的蛋白酪氨酸激酶(PTK)抑制剂的3-氰基-6-烷氧基-7-硝基-4-喹诺酮中间体的方法:其中 R是通过使取代的邻氨基苯甲酸酯与N,N-二甲基甲酰胺二甲基缩醛反应制得的烷基(C 1 -C 3 -C 3),得到与t缩合的N,N-二甲基脒 (2-氰基-2-叔丁氧基羰基乙烯基)邻氨基苯甲酸酯,将其水解,得到N-(2-氰基-2-羧基乙烯基)邻氨基苯甲酸酯,然后脱羧,得到N-(2-氰基-2- -2-羧基乙烯基)邻氨基苯甲酸甲酯,然后环化,得到3-氰基-6-烷氧基-7-硝基-4-喹诺酮。