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    Production process of optically active 3-quinuclidinol derivative
    1.
    发明授权
    Production process of optically active 3-quinuclidinol derivative 有权
    光学活性3-奎宁环衍生物的制备方法

    公开(公告)号：US08436181B2

    公开(公告)日：2013-05-07

    申请号：US12676301

    申请日：2008-09-02

    申请人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    发明人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    IPC分类号： A61K31/44 ,  C07D453/02

    CPC分类号： C07D453/02 ,  B01J31/1805 ,  B01J31/2409 ,  B01J2231/643 ,  B01J2531/0266 ,  B01J2531/821 ,  C07B53/00

    摘要： A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).

    摘要翻译： 提供了使用容易获得的钌化合物作为不对称还原催化剂有效地制备高光学纯度的光学活性的3-奎宁环醇衍生物的方法。 该方法是制备由下式（III）表示的光学活性3-奎宁环醇衍生物的方法，包括在下述式（I）表示的钌化合物（II）的存在下，使下式（I）表示的3-奎宁环酮衍生物 式（II）：Ru（X）（Y）（Px）n [R1R2C *（NR3R4）-A-R5R6C *（NR7R8）]（式中，R表示氢原子或C7〜C18芳烷基等 ，X和Y表示氢原子或卤素原子等，Px表示膦配体，n表示1或2，R1〜R8表示氢原子或C1〜C20烷基等，*表示光学活性碳原子， A表示亚乙基等）。

    Production process of optically active 3-quinuclidinol derivative
    2.
    发明授权
    Production process of optically active 3-quinuclidinol derivative 有权
    光学活性3-奎宁环衍生物的制备方法

    公开(公告)号：US08759524B2

    公开(公告)日：2014-06-24

    申请号：US13858586

    申请日：2013-04-08

    申请人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    发明人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    IPC分类号： C07D453/02

    CPC分类号： C07D453/02 ,  B01J31/1805 ,  B01J31/2409 ,  B01J2231/643 ,  B01J2531/0266 ,  B01J2531/821 ,  C07B53/00

    摘要： A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).

    摘要翻译： 提供了使用容易获得的钌化合物作为不对称还原催化剂有效地制备高光学纯度的光学活性的3-奎宁环醇衍生物的方法。 该方法是制备由下式（III）表示的光学活性3-奎宁环醇衍生物的方法，包括在下述式（I）表示的钌化合物（II）的存在下，使下式（I）表示的3-奎宁环酮衍生物 式（II）：Ru（X）（Y）（Px）n [R1R2C *（NR3R4）-A-R5R6C *（NR7R8）]（式中，R表示氢原子或C7〜C18芳烷基等 ，X和Y表示氢原子或卤素原子等，Px表示膦配体，n表示1或2，R1〜R8表示氢原子或C1〜C20烷基等，*表示光学活性碳原子， A表示亚乙基等）。

    PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE
    3.
    发明申请
    PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE 有权
    光活性3-喹啉二醇衍生物的生产工艺

    公开(公告)号：US20100174081A1

    公开(公告)日：2010-07-08

    申请号：US12676301

    申请日：2008-09-02

    申请人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    发明人： Takeshi Ohkuma ,  Noriyoshi Arai ,  Masaya Akashi ,  Hirohito Oooka ,  Tsutomu Inoue

    IPC分类号： C07D453/02

    CPC分类号： C07D453/02 ,  B01J31/1805 ,  B01J31/2409 ,  B01J2231/643 ,  B01J2531/0266 ,  B01J2531/821 ,  C07B53/00

    摘要： A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).

    摘要翻译： 提供了使用容易获得的钌化合物作为不对称还原催化剂有效地制备高光学纯度的光学活性的3-奎宁环醇衍生物的方法。 该方法是制备由下式（III）表示的光学活性3-奎宁环醇衍生物的方法，包括在下述式（I）表示的钌化合物（II）的存在下，使下式（I）表示的3-奎宁环酮衍生物 式（II）：Ru（X）（Y）（Px）n [R1R2C *（NR3R4）-A-R5R6C *（NR7R8）]（式中，R表示氢原子或C7〜C18芳烷基等 ，X和Y表示氢原子或卤素原子等，Px表示膦配体，n表示1或2，R1〜R8表示氢原子或C1〜C20烷基等，*表示光学活性碳原子， A表示亚乙基等）。