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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 有权
    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：US20100105922A1

    公开(公告)日：2010-04-29

    申请号：US12648022

    申请日：2009-12-28

    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： C07D233/64 ,  C07C27/04

    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
    2.
    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 the preparation of imidazole derivatives
    8.
    发明授权
    Process for the preparation of imidazole derivatives 失效
    咪唑衍生物的制备方法

    公开(公告)号：US06713632B1

    公开(公告)日：2004-03-30

    申请号：US10019094

    申请日：2002-04-12

    申请人： Jun-ichi Kawakami

    发明人： Jun-ichi Kawakami

    IPC分类号： C07P23354

    CPC分类号： C07D233/64

    摘要： A method for producing a compound of the formula: wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group and ring A is an imidazole ring which is optionally substituted further, or a salt thereof, which method comprises reacting a compound of the formula: wherein ring A is as defined above, or a salt thereof, and a compound of the formula: R—M1  (II) wherein M1 is an alkali metal atom or a group of the formula: —Mg—Y1 where Y1 is a halogen atom, and R is as defined above, or a salt thereof, and bringing the resulting product into contact with an acid.

    摘要翻译： 一种制备下式化合物的方法：其中R是任选取代的烃基或任选取代的杂环基，而环A是进一步任选被取代的咪唑环，或其盐，该方法包括使 式：其中环A如上所定义，或其盐，和下式化合物：其中M 1是碱金属原子或式-Mg-Y 1的基团，其中Y 1 >是卤素原子，R如上定义，或其盐，并使所得产物与酸接触。