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1. 发明申请

US20050043544A1 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
标题翻译：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。

2. 发明申请

US20120077985A1 PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME 失效
标题翻译：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。

3. 发明授权

US08586762B2 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
标题翻译：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：US08586762B2
公开(公告)日：2013-11-19
申请号：US13305411
申请日：2011-11-28
申请人： Jun-Ichi Kawakami , Shigeru Nuwa , Miki Shokyo
发明人： Jun-Ichi Kawakami , Shigeru Nuwa , Miki Shokyo
IPC分类号： C07D235/02
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):
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：

4. 发明授权

US08093403B2 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 有权
标题翻译：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。

5. 发明授权

US07662974B2 Process for producing fused imidazole compound, reformatsky reagent in stable form, and process for producing the same 失效
标题翻译：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。

6. 发明申请

US20100105922A1 PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME 有权
标题翻译：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。

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