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    Processes for the production of thienopyrimidine derivatives
    3.
    发明授权
    Processes for the production of thienopyrimidine derivatives 失效
    噻吩并嘧啶衍生物的制备方法

    公开(公告)号：US06849738B2

    公开(公告)日：2005-02-01

    申请号：US10220233

    申请日：2001-02-27

    申请人： Koichiro Fukuoka ,  Hiroaki Yamamoto ,  Kazuhiro Kimura ,  Junichi Kawakami ,  Shokyo Miki

    发明人： Koichiro Fukuoka ,  Hiroaki Yamamoto ,  Kazuhiro Kimura ,  Junichi Kawakami ,  Shokyo Miki

    IPC分类号： C07D333/38 ,  C07D495/04

    CPC分类号： C07D495/04 ,  C07D333/38

    摘要： The present invention provides a process for producing an intermediate for thienopyrimidine derivatives having the GnRH antagonistic activity at an industrial large scale.The process for production of the present invention relates to a process for producing a compound represented by the formula (III): wherein respective symbols have the same meanings as those described below, or a salt thereof, which comprises subjecting a compound represented by the formula (I): wherein R1 denotes hydrogen, nitro, halogen, phthalimido, mono- or di-(alkylcarbonyl)amino or alkoxy, or a salt thereof, to an acid halogenating reaction, which is successively reacted with malonic acid ester and magnesium alkoxide, treated with an acid, and reacted with sulfur and a compound represented by the formula: NCCH2COOR2 [wherein R2 denotes alkyl or aryl], or a salt thereof, in the presence of primary amine. According to the process of production of the present invention, thienopyrimidine derivatives having the GnRH antagonistic activity can be produced effectively and at an industrial large scale by a high yield and simple method.

    摘要翻译： 本发明提供了一种在工业上大规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物的中间体的方法。本发明的制备方法涉及一种由式（III）表示的化合物的制备方法：其中各自 符号具有与下述相同的含义或其盐，其包括使由式（I）表示的化合物：其中R 1表示氢，硝基，卤素，苯二甲酰亚氨基，单 - 或二 - （烷基羰基） 氨基或烷氧基或其盐与酸卤化反应反应，该酸卤化反应与丙酸和烷氧基镁连续反应，用酸处理，并与硫和式NCCH 2 COOR 2表示的化合物反应[其中 R 2表示烷基或芳基]或其盐，在伯胺的存在下。 根据本发明的制造方法，可以通过高产率和简单的方法有效地以工业规模生产具有GnRH拮抗活性的噻吩并嘧啶衍生物。

    Process for preparation of benzylpiperidine compounds
    4.
    发明授权
    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：US07049441B2

    公开(公告)日：2006-05-23

    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： C07D211/70

    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，烷氧基 任选具有取代基的基团或任选具有取代基的杂环基，R 3是低级烷基。

    PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME
    5.
    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
    6.
    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
    7.
    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
    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。