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    PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME
    1.
    发明申请
    PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME 失效
    制备熔融咪唑化合物的方法，稳定形式的改性试剂及其制备方法

    公开(公告)号：US20120077985A1

    公开(公告)日：2012-03-29

    申请号：US13305411

    申请日：2011-11-28

    申请人： Jun-ichi Kawakami ,  Shigeru Nuwa ,  Shokyo Miki

    发明人： Jun-ichi Kawakami ,  Shigeru Nuwa ,  Shokyo Miki

    IPC分类号： C07D403/04

    CPC分类号： C07D233/64 ,  C07D487/04 ,  C07F3/06

    摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

    摘要翻译： 本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法; 和一种适用于该方法的稳定形式的Reformatsky试剂。 在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐 和金属卤化物，然后使其进行闭环反应。 在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same
    5.
    发明授权
    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 有权
    稠合咪唑化合物的制备方法，稳定形式的重格列烷基试剂及其制备方法

    公开(公告)号：US08093403B2

    公开(公告)日：2012-01-10

    申请号：US12648022

    申请日：2009-12-28

    申请人： Jun-Ichi Kawakami ,  Shigeru Nuwa ,  Shokyo Miki

    发明人： Jun-Ichi Kawakami ,  Shigeru Nuwa ,  Shokyo Miki

    IPC分类号： C07D233/64

    CPC分类号： C07D233/64 ,  C07D487/04 ,  C07F3/06

    摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I); and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

    摘要翻译： 本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法; 和一种适用于该方法的稳定形式的Reformatsky试剂。 在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐 和金属卤化物，然后使其进行闭环反应。 在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same
    6.
    发明授权
    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
    稠合咪唑化合物的制备方法，稳定形式的重格列烷基试剂及其制备方法

    公开(公告)号：US07662974B2

    公开(公告)日：2010-02-16

    申请号：US10500999

    申请日：2003-01-09

    申请人： Jun-ichi Kawakami ,  Koji Nakamoto ,  Shigeru Nuwa ,  Syoji Handa ,  Shokyo Miki

    发明人： Jun-ichi Kawakami ,  Koji Nakamoto ,  Shigeru Nuwa ,  Syoji Handa ,  Shokyo Miki

    IPC分类号： C07F3/06

    CPC分类号： C07D233/64 ,  C07D487/04 ,  C07F3/06

    摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

    摘要翻译： 本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法：和适于该方法的稳定形式的Reformatsky试剂。 在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐， 金属卤化物，然后使其进行闭环反应。 在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same
    9.
    发明申请
    Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
    稠合咪唑化合物的制备方法，稳定形式的重格列烷基试剂及其制备方法

    公开(公告)号：US20050043544A1

    公开(公告)日：2005-02-24

    申请号：US10500999

    申请日：2003-01-09

    申请人： Shigeru Nuwa ,  Syoji Handa ,  Shokyo Miki

    发明人： Shigeru Nuwa ,  Syoji Handa ,  Shokyo Miki

    IPC分类号： C07D233/64 ,  A61K31/4164 ,  A61K31/4188 ,  A61P13/08 ,  A61P15/00 ,  A61P17/14 ,  A61P35/00 ,  A61P43/00 ,  C07D213/55 ,  C07D215/12 ,  C07D233/54 ,  C07D307/16 ,  C07D307/33 ,  C07D487/04 ,  C07F3/06 ,  C07D233/00 ,  C09K19/00

    CPC分类号： C07D233/64 ,  C07D487/04 ,  C07F3/06

    摘要： The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

    摘要翻译： 本发明提供了用于生产由通式（I）表示的类固醇C17,20裂解酶抑制剂的工业上有利的方法：和适于该方法的稳定形式的Reformatsky试剂。 在本发明中，通式（I）表示的化合物是通过在金属氢化物络合物的存在下，通过在Reformatsky反应中还原由特定的羰基化合物得到的特定的β-羟基酯化合物衍生物或其盐， 金属卤化物，然后使其进行闭环反应。 在上述Reformatsky反应中，使用由通式BrZnCH 2 COOC 2 H 5表示的化合物或由式（BrZnCH2COOC2H5.THF）2表示的化合物的晶体的稳定溶液是有用的。

    Process for preparation of benzylpiperidine compounds
    10.
    发明申请
    Process for preparation of benzylpiperidine compounds 失效
    苄基哌啶化合物的制备方法

    公开(公告)号：US20050038257A1

    公开(公告)日：2005-02-17

    申请号：US10939293

    申请日：2004-09-10

    申请人： Shokyo Miki ,  Mitsuhiro Takeda ,  Koji Nakamoto

    发明人： Shokyo Miki ,  Mitsuhiro Takeda ,  Koji Nakamoto

    IPC分类号： C07D211/34 ,  C07D211/62 ,  C07D211/70 ,  C07D211/96 ,  C07F9/40 ,  C07D41/02 ,  C07D211/82

    CPC分类号： C07D401/12 ,  C07D211/34 ,  C07D211/62 ,  C07D211/70 ,  C07D211/96 ,  C07F9/094 ,  C07F9/4056 ,  Y02P20/55

    摘要： According to the process as shown in the following scheme having a step for reacting Compound (I) with Compound (II) to produce Compound (III), benzylpiperidine compounds useful as synthesis starting materials of pharmaceutical agents, agricultural chemicals and the like can be produced conveniently by a short step: wherein R1 is a hydrogen atom or an amino-protecting group, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, and R3 is a lower alkyl group.

    摘要翻译： 根据具有使化合物（I）与化合物（II）反应生成化合物（III）的步骤的方法所示的方法，可以制备用作药剂，农药等的合成原料的苄基哌啶化合物 方便地通过短步骤：其中R 1是氢原子或氨基保护基，R 2是氢原子，任选具有取代基的烃基，任选具有取代基的烷氧基或任选具有取代基的杂环基 取代基，R 3为低级烷基。