Process for production of 4(3H)-quinazolinone derivative
    8.
    发明申请
    Process for production of 4(3H)-quinazolinone derivative 审中-公开
    制备4(3H) - 喹唑啉酮衍生物的方法

    公开(公告)号:US20090306375A1

    公开(公告)日:2009-12-10

    申请号:US11921726

    申请日:2006-06-07

    IPC分类号: C07D239/72

    CPC分类号: C07D401/12

    摘要: The present invention provides a process for producing a 4(3H)-quinazolinone derivative, which is useful as a medicinal substance, with better efficiency in an industrial scale. The process comprises the steps of reacting 4-hydroxy-N-tert-butoxycarbonylpiperidine with 4-fluoro-1-nitrobenzene in the presence of sodium hydride, reacting the resulting product with cyclobutanone, reducing the resulting product to give 4-(1-cyclobutyl-4-piperidinyl)oxyaniline, and reacting this compound with 2-methyl-5-trifluoromethyl-4H-3,1-benzoxazin-4-one to give 3-{4-[(1-cyclobutyl-4-piperidinyl)oxy]phenyl}-2-methyl-5-trifluoromethyl-4(3H)-quinazolinone.

    摘要翻译: 本发明提供一种可用作药物的4(3H) - 喹唑啉酮衍生物的方法,其工业规模效率更好。 该方法包括在氢化钠存在下使4-羟基-N-叔丁氧基羰基哌啶与4-氟-1-硝基苯反应的步骤,使所得产物与环丁酮反应,将所得产物还原得到4-(1-环丁基 -4-哌啶基)氧苯胺,并使该化合物与2-甲基-5-三氟甲基-4H-3,1-苯并恶嗪-4-酮反应,得到3- {4 - [(1-环丁基-4-哌啶基)氧基] 苯基} -2-甲基-5-三氟甲基-4(3H) - 喹唑啉酮。