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    Process for production of 4(3H)-quinazolinone derivative
    1.
    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

    申请人： Satoshi Kii ,  Tsuyoshi Nagase ,  Kimihiko Sato ,  Nagaaki Sato ,  Naotaka Sawada ,  Takayuki Tsuritani

    发明人： Satoshi Kii ,  Tsuyoshi Nagase ,  Kimihiko Sato ,  Nagaaki Sato ,  Naotaka Sawada ,  Takayuki Tsuritani

    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。

    PROCESS FOR PREPARING AMINOADAMANTYL CARBAMATE DERIVATIVES
    2.
    发明申请
    PROCESS FOR PREPARING AMINOADAMANTYL CARBAMATE DERIVATIVES 有权
    制备氨基甲酰胺氨基甲酸酯衍生物的方法

    公开(公告)号：US20130197240A1

    公开(公告)日：2013-08-01

    申请号：US13816120

    申请日：2011-08-08

    申请人： Yutaka Nishino ,  Hideki Shimizu ,  Takayuki Tsuritani ,  Natsuko Suzuki ,  Mutsumi Takaki ,  Tatsuya Kobayashi ,  Hideaki Sakamoto

    发明人： Yutaka Nishino ,  Hideki Shimizu ,  Takayuki Tsuritani ,  Natsuko Suzuki ,  Mutsumi Takaki ,  Tatsuya Kobayashi ,  Hideaki Sakamoto

    IPC分类号： C07D231/14

    CPC分类号： C07D231/14 ,  A61K31/415 ,  C07B2200/07 ,  C07C269/02 ,  C07C269/06 ,  C07C269/08 ,  C07C271/34 ,  C07C2603/74

    摘要： Disclosed is a process for producing an aminoadamantane carbamate derivative which is useful as a significant intermediate of an 11βHSD-1 inhibitor.A process for producing an acid addition salt of a compound represented by the Formula (II): or a solvate of the acid addition salt, wherein R1 and R2 are each independently hydrogen, substituted or unsubstituted alkyl or the like; R3 and R4 are each independently hydrogen, substituted or unsubstituted alkyl or the like; and R5 and R6 are each independently hydrogen, halogen, carboxy, nitro, substituted or unsubstituted alkyl or the like; which comprises separating an acid addition salt of a compound represented by the Formula (II) or a solvate of the acid addition salt by adding an acid to a mixture of syn isomer and anti isomer of a compound represented by the Formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined above, in the presence of a solvent.

    摘要翻译： 公开了一种生产氨基金刚烷氨基甲酸酯衍生物的方法，其可用作11betaHSD-1抑制剂的重要中间体。 一种由式（II）表示的化合物的酸加成盐或其酸加成盐的溶剂化物的方法，其中R1和R2各自独立地为氢，取代或未取代的烷基等; R 3和R 4各自独立地为氢，取代或未取代的烷基等; R 5和R 6各自独立地为氢，卤素，羧基，硝基，取代或未取代的烷基等; 其包括通过向由式（I）表示的化合物的顺式异构体和反式异构体的混合物中加入酸来分离由式（II）表示的化合物的酸加成盐或酸加成盐的溶剂合物：其中 在溶剂的存在下，R 1，R 2，R 3，R 4，R 5和R 6如上定义。

    Process for preparing aminoadamantyl carbamate derivatives
    4.
    发明授权
    Process for preparing aminoadamantyl carbamate derivatives 有权
    氨基甲酰胺基氨基甲酸酯衍生物的制备方法

    公开(公告)号：US08901316B2

    公开(公告)日：2014-12-02

    申请号：US13816120

    申请日：2011-08-08

    申请人： Yutaka Nishino ,  Hideki Shimizu ,  Takayuki Tsuritani ,  Natsuko Suzuki ,  Mutsumi Takaki ,  Tatsuya Kobayashi ,  Hideaki Sakamoto

    发明人： Yutaka Nishino ,  Hideki Shimizu ,  Takayuki Tsuritani ,  Natsuko Suzuki ,  Mutsumi Takaki ,  Tatsuya Kobayashi ,  Hideaki Sakamoto

    IPC分类号： C07C269/06 ,  C07C269/08 ,  C07C271/34 ,  C07D231/14 ,  C07C269/02 ,  A61K31/415

    CPC分类号： C07D231/14 ,  A61K31/415 ,  C07B2200/07 ,  C07C269/02 ,  C07C269/06 ,  C07C269/08 ,  C07C271/34 ,  C07C2603/74

    摘要： Disclosed is a process for producing an aminoadamantane carbamate derivative which is useful as a significant intermediate of an 11βHSD-1 inhibitor.A process for producing an acid addition salt of a compound represented by the Formula (II): or a solvate of the acid addition salt, wherein R1 and R2 are each independently hydrogen, substituted or unsubstituted alkyl or the like; R3 and R4 are each independently hydrogen, substituted or unsubstituted alkyl or the like; and R5 and R6 are each independently hydrogen, halogen, carboxy, nitro, substituted or unsubstituted alkyl or the like; which comprises separating an acid addition salt of a compound represented by the Formula (II) or a solvate of the acid addition salt by adding an acid to a mixture of syn isomer and anti isomer of a compound represented by the Formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined above, in the presence of a solvent.

    摘要翻译： 公开了一种生产氨基丁基氨基甲酸酯衍生物的方法，其可用作11重量％HSD-1抑制剂的重要中间体。 一种由式（II）表示的化合物的酸加成盐或其酸加成盐的溶剂化物的方法，其中R1和R2各自独立地为氢，取代或未取代的烷基等; R 3和R 4各自独立地为氢，取代或未取代的烷基等; R 5和R 6各自独立地为氢，卤素，羧基，硝基，取代或未取代的烷基等; 其包括通过向由式（I）表示的化合物的顺式异构体和反式异构体的混合物中加入酸来分离由式（II）表示的化合物的酸加成盐或酸加成盐的溶剂合物：其中 在溶剂的存在下，R 1，R 2，R 3，R 4，R 5和R 6如上定义。