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    Methods for producing cyclic benzamidine derivatives
    1.
    发明申请
    Methods for producing cyclic benzamidine derivatives 失效
    环苯甲脒衍生物的制备方法

    公开(公告)号：US20060058370A1

    公开(公告)日：2006-03-16

    申请号：US11208289

    申请日：2005-08-18

    申请人： Naoyuki Shimomura ,  Manabu Sasho ,  Akio Kayano ,  Kazuhiro Yoshizawa ,  Masahiko Tsujii ,  Hiroshi Kuroda ,  Ken Furukawa

    发明人： Naoyuki Shimomura ,  Manabu Sasho ,  Akio Kayano ,  Kazuhiro Yoshizawa ,  Masahiko Tsujii ,  Hiroshi Kuroda ,  Ken Furukawa

    IPC分类号： C07D209/44 ,  A61K31/4035

    CPC分类号： C07D295/096 ,  C07C43/225 ,  C07C43/315 ,  C07C255/54 ,  C07C255/56 ,  C07C303/28 ,  C07D209/44 ,  C07D209/48 ,  C07C309/66

    摘要： In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

    摘要翻译： 在本发明中，制备氟化环状苯甲脒衍生物（A）或其盐的方法包括使特定的新化合物与氨或酰亚胺反应的步骤。 本发明用于生产吗啉取代的苯甲酰甲基衍生物（B）或其盐的方法包括特异性新化合物与吗啉的反应，产物与卤化试剂的反应和产物的脱缩合作用。 本发明的制备环状苯甲脒衍生物（C）或其盐的方法包括将化合物（A）或其盐与化合物（B）或其盐偶联的步骤在 醚或烃。 本发明用于环状苄脒衍生物（C）或其盐的重结晶的方法包括将化合物（C）或其盐溶解在包含醇和水的混合溶剂中的步骤或包含 醚和水，溶解后加入另外的水，使化合物（C）的结晶或其盐析出。

    Methods for producing cyclic benzamidine derivatives
    2.
    发明授权
    Methods for producing cyclic benzamidine derivatives 失效
    环苯甲脒衍生物的制备方法

    公开(公告)号：US07375236B2

    公开(公告)日：2008-05-20

    申请号：US11208289

    申请日：2005-08-18

    申请人： Naoyuki Shimomura ,  Manabu Sasho ,  Akio Kayano ,  Kazuhiro Yoshizawa ,  Masahiko Tsujii ,  Hiroshi Kuroda ,  Ken Furukawa

    发明人： Naoyuki Shimomura ,  Manabu Sasho ,  Akio Kayano ,  Kazuhiro Yoshizawa ,  Masahiko Tsujii ,  Hiroshi Kuroda ,  Ken Furukawa

    IPC分类号： C07D265/30 ,  C07D209/44 ,  C07C43/307

    CPC分类号： C07D295/096 ,  C07C43/225 ,  C07C43/315 ,  C07C255/54 ,  C07C255/56 ,  C07C303/28 ,  C07D209/44 ,  C07D209/48 ,  C07C309/66

    摘要： In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide.The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product.The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon.The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

    摘要翻译： 在本发明中，制备氟化环状苯甲脒衍生物（A）或其盐的方法包括使特定的新化合物与氨或酰亚胺反应的步骤。 本发明用于生产吗啉取代的苯甲酰甲基衍生物（B）或其盐的方法包括特异性新化合物与吗啉的反应，产物与卤化试剂的反应和产物的脱缩合作用。 本发明的制备环状苯甲脒衍生物（C）或其盐的方法包括将化合物（A）或其盐与化合物（B）或其盐偶联的步骤在 醚或烃。 本发明用于环状苄脒衍生物（C）或其盐的重结晶的方法包括将化合物（C）或其盐溶解在包含醇和水的混合溶剂中的步骤或包含 醚和水，溶解后加入另外的水，使化合物（C）的结晶或其盐析出。

    Process for production of pyrazole-fused ring derivatives
    3.
    发明授权
    Process for production of pyrazole-fused ring derivatives 失效
    吡唑稠环衍生物的制备方法

    公开(公告)号：US07858809B2

    公开(公告)日：2010-12-28

    申请号：US11578134

    申请日：2005-04-08

    申请人： Shigeto Negi ,  Toshikazu Shimizu ,  Hiroshi Kuroda ,  Naoyuki Shimomura ,  Manabu Sasho ,  Yorihisa Hoshino ,  Manabu Kuboto

    发明人： Shigeto Negi ,  Toshikazu Shimizu ,  Hiroshi Kuroda ,  Naoyuki Shimomura ,  Manabu Sasho ,  Yorihisa Hoshino ,  Manabu Kuboto

    IPC分类号： C07D231/54

    CPC分类号： C07D471/04

    摘要： Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.

    摘要翻译： 用于合成吡唑稠合环衍生物如7-苯基吡唑并[1,5-a]吡啶衍生物的中间体及其制备方法。 制备由通式（II）表示的化合物的方法，其中Z1和Z2各自独立地表示次甲基或氮原子; R1表示乙基等; R5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等，其盐或两者的溶剂合物，包括以下步骤：使通式（I）表示的化合物与其反应，其中Z1，Z2，R5，R1， R2和R3各自具有与上述相同的定义，与有机金属试剂; 然后使所得产物与五氟碘苯反应。

    Process for production of pyrazole-fused ring derivatives
    4.
    发明申请
    Process for production of pyrazole-fused ring derivatives 失效
    吡唑稠环衍生物的制备方法

    公开(公告)号：US20070191613A1

    公开(公告)日：2007-08-16

    申请号：US11578134

    申请日：2005-04-08

    申请人： Shigeto Negi ,  Toshikazu Shimizu ,  Hiroshi Kuroda ,  Naoyuki Shimomura ,  Manabu Sasho ,  Yorihisa Hoshino ,  Manabu Kubota

    发明人： Shigeto Negi ,  Toshikazu Shimizu ,  Hiroshi Kuroda ,  Naoyuki Shimomura ,  Manabu Sasho ,  Yorihisa Hoshino ,  Manabu Kubota

    IPC分类号： C07D231/54

    CPC分类号： C07D471/04

    摘要： An object of the invention is to find out intermediates usful for the synthesis of pyrazol-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a method for producing the same. A method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; R1 represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.

    摘要翻译： 本发明的目的是找出有用于合成吡唑稠合环衍生物（如7-苯基吡唑并[1,5-a]吡啶衍生物）的中间体及其制备方法。 由通式（II）表示的化合物，其中Z 1和Z 2各自独立地表示次甲基或氮原子的方法; R 1表示乙基等; R 5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等，其盐或两者的溶剂合物，包括 步骤：使通式（I）表示的化合物，其中Z 1，Z 2，R 5，R 5， 1，R 2和R 3各自具有与上述相同的定义与有机金属试剂; 然后使所得产物与五氟碘苯反应。