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1. 发明申请

US20080306283A1 Process For Production of Aralkyloxypyrrolidine Derivative 有权
标题翻译：芳基吡咯烷衍生物的制备方法
公开(公告)号：US20080306283A1
公开(公告)日：2008-12-11
申请号：US11990766
申请日：2006-08-22
申请人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
发明人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译：本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。

2. 发明申请

US20110224444A1 PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权
标题翻译：制备阿拉克氧基吡咯烷衍生物的方法
公开(公告)号：US20110224444A1
公开(公告)日：2011-09-15
申请号：US13115385
申请日：2011-05-25
申请人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
发明人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
IPC分类号： C07D207/12 , C07D207/00
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译：本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。

3. 发明申请

US20070292926A1 Processes for Producing Optically Active 1-Substituted 2-Methylpyrrolidine and Intermediate Therefor 失效
标题翻译：用于生产光学活性1-取代的2-甲基吡咯烷及其中间体的方法
公开(公告)号：US20070292926A1
公开(公告)日：2007-12-20
申请号：US10586337
申请日：2005-01-19
申请人： Akira Nishiyama , Naoaki Taoka , Narumi Kishimoto , Nobuo Nagashima
发明人： Akira Nishiyama , Naoaki Taoka , Narumi Kishimoto , Nobuo Nagashima
IPC分类号： C12P7/18 , C07C31/20 , C07D207/04
CPC分类号： C12P17/10 , C07C303/28 , C12P7/18 , C12P11/00 , C07C309/66
摘要： The present invention relates to a process for producing an optically active 1,4-pentanediol by asymmetrically reducing 5-hydroxy-2-pentanone, which is easily available at low cost. The present invention also relates to a process for producing an optically active 1-substituted 2-methylpyrrolidine including sulfonylating the optically active 1,4-pentanediol to convert it to an optically active sulfonate compound, and reacting the compound with an amine. According to the processes of the present invention, an optically active 1,4-pentanediol and an optically active 1-substituted 2-methylpyrrolidine, which are useful as an intermediate for medicines and an intermediate for agricultural chemicals, can be simply produced from an inexpensive starting material.
摘要翻译：本发明涉及通过不对称地还原5-羟基-2-戊酮来制备光学活性的1,4-戊二醇的方法，该方法容易以低成本获得。本发明还涉及一种光学活性1-取代的2-甲基吡咯烷的制备方法，其包括使光学活性的1,4-戊二醇磺酰化以将其转化成光学活性的磺酸盐化合物，并使该化合物与胺反应。根据本发明的方法，用作药物中间体和农药中间体的光学活性的1,4-丁二醇和光学活性的1-取代的2-甲基吡咯烷可以简便地从廉价的起始材料

4. 发明申请

US20090312577A1 Process for Production of Beta-Amino-Alpha-Hydroxy Carbonxamide Derivative 失效
标题翻译： β-氨基-α-羟基碳酰胺衍生物的制备方法
公开(公告)号：US20090312577A1
公开(公告)日：2009-12-17
申请号：US12223036
申请日：2007-01-16
申请人： Narumi Kishimoto , Hiroaki Yasukouchi , Toshihiro Takeda
发明人： Narumi Kishimoto , Hiroaki Yasukouchi , Toshihiro Takeda
IPC分类号： C07C237/06
CPC分类号： C07C231/12 , C07B2200/07 , C07C231/16 , C07C2601/02 , C07C237/04
摘要： Provided is a process for production of a β-amino-α-hydroxy carboxamide derivative that is important in production of drugs or the like. In the presence of a predetermined solvent, a β-(N-protected)amino-α-hydroxycarboxylic acid is reacted with an amine to conversion to a β-(N-protected)amino-α-hydroxy carboxamide derivative; then the derivative is deprotected for conversion to a β-amino-α-hydroxy carboxamide derivative; and the derivative is crystallized using a protic solvent to obtain a crystal. The high-purity β-amino-α-hydroxy carboxamide derivative can be stably produced on an industrial scale by the process.
摘要翻译：本发明提供了生产药物等中重要的β-氨基-α-羟基甲酰胺衍生物的生产方法。在预定溶剂的存在下，将β-（N-保护的）氨基-α-羟基羧酸与胺反应以转化为β-（N-保护的）氨基-α-羟基甲酰胺衍生物; 然后将衍生物去保护以转化成β-氨基-α-羟基甲酰胺衍生物; 并使用质子性溶剂使衍生物结晶，得到结晶。高纯度β-氨基-α-羟基甲酰胺衍生物可以通过该工艺在工业规模上稳定地生产。

5. 发明授权

US07408084B2 Process for producing optically active β-amino alcohol 失效
标题翻译：光学活性β-氨基醇的制备方法
公开(公告)号：US07408084B2
公开(公告)日：2008-08-05
申请号：US10516469
申请日：2003-06-02
申请人： Akira Nishiyama , Narumi Kishimoto , Nobuo Nagashima
发明人： Akira Nishiyama , Narumi Kishimoto , Nobuo Nagashima
IPC分类号： C07C211/05 , C07C213/08
CPC分类号： C07C49/84 , C07B2200/07 , C07C45/63 , C07C213/00 , C07C215/28 , C07C221/00 , C07C215/30 , C07C225/16
摘要： A process for easily producing an optically active β-amino alcohol useful as a pharmaceutical intermediate from an inexpensive, readily available starting material is provided. A readily available α-substituted ketone is reacted with an optically active amine to yield a diastereomer mixture of an optically active α-substituted aminoketone. One of the diastereomers is isolated optionally after the diastereomers are converted to salts with an acid. The optically active α-substituted aminoketone or a salt thereof thus isolated was stereoselectively reduced to yield an optically active β-substituted amino alcohol. The optically active β-substituted amino alcohol is subjected to hydrogenolysis to produce an optically active β-amino alcohol or a salt thereof.
摘要翻译：提供了一种从便宜的，容易获得的起始材料中容易地生产用作药物中间体的光学活性β-氨基醇的方法。将容易获得的α-取代的酮与光学活性胺反应，得到光学活性的α-取代的氨基酮的非对映异构体混合物。在非对映异构体与酸转化成盐之后，任选地分离非对映异构体之一。将如此分离的光学活性α-取代的氨基酮或其盐立体选择性地还原，得到光学活性的β-取代的氨基醇。将光学活性的β-取代氨基醇进行氢解以产生光学活性的β-氨基醇或其盐。

6. 发明申请

US20050277791A1 Process for producing optically active beta-amino alcohol 失效
标题翻译：光学活性β-氨基醇的制备方法
公开(公告)号：US20050277791A1
公开(公告)日：2005-12-15
申请号：US10516469
申请日：2003-06-02
申请人： Akira Nishiyama , Narumi Kishimoto , Nobuo Nagashima
发明人： Akira Nishiyama , Narumi Kishimoto , Nobuo Nagashima
IPC分类号： C07C45/63 , C07C49/84 , C07C213/00 , C07C215/28 , C07C215/30 , C07C221/00 , C07C225/16 , C07C29/06
CPC分类号： C07C49/84 , C07B2200/07 , C07C45/63 , C07C213/00 , C07C215/28 , C07C221/00 , C07C215/30 , C07C225/16
摘要： A process for easily producing an optically active β-amino alcohol useful as a pharmaceutical intermediate from an inexpensive, readily available starting material is provided. A readily available α-substituted ketone is reacted with an optically active amine to yield a diastereomer mixture of an optically active α-substituted aminoketone. One of the diastereomers is isolated optionally after the diastereomers are converted to salts with an acid. The optically active α-substituted aminoketone or a salt thereof thus isolated was stereoselectively reduced to yield an optically active β-substituted amino alcohol. The optically active β-substituted amino alcohol is subjected to hydrogenolysis to produce an optically active β-amino alcohol or a salt thereof.
摘要翻译：提供了一种从便宜的，容易获得的起始材料中容易地生产用作药物中间体的光学活性β-氨基醇的方法。将容易获得的α-取代的酮与光学活性胺反应，得到光学活性的α-取代的氨基酮的非对映异构体混合物。在非对映异构体与酸转化成盐之后，任选地分离非对映异构体之一。将如此分离的光学活性α-取代的氨基酮或其盐立体选择性地还原，得到光学活性的β-取代的氨基醇。将光学活性的β-取代氨基醇进行氢解以产生光学活性的β-氨基醇或其盐。

7. 发明授权

US08183413B2 Process for production of β-amino-α-hydroxy carboxamide derivative 失效
标题翻译： α-氨基-α-羟基甲酰胺衍生物的制备方法
公开(公告)号：US08183413B2
公开(公告)日：2012-05-22
申请号：US12223036
申请日：2007-01-16
申请人： Narumi Kishimoto , Hiroaki Yasukouchi , Toshihiro Takeda
发明人： Narumi Kishimoto , Hiroaki Yasukouchi , Toshihiro Takeda
IPC分类号： C07C231/02
CPC分类号： C07C231/12 , C07B2200/07 , C07C231/16 , C07C2601/02 , C07C237/04
摘要： Provided is a process for production of a β-amino-α-hydroxy carboxamide derivative that is important in production of drugs or the like. In the presence of a predetermined solvent, a β-(N-protected)amino-α-hydroxycarboxylic acid is reacted with an amine to conversion to a β-(N-protected)amino-α-hydroxy carboxamide derivative; then the derivative is deprotected for conversion to a β-amino-α-hydroxy carboxamide derivative; and the derivative is crystallized using a protic solvent to obtain a crystal. The high-purity β-amino-α-hydroxy carboxamide derivative can be stably produced on an industrial scale by the process.
摘要翻译：本发明提供了生产药物等中重要的α-氨基-α-羟基甲酰胺衍生物的制备方法。在预定溶剂的存在下，将（N-保护的）氨基-α-羟基羧酸与胺反应以转化为 - （N-保护的）氨基-α-羟基羧酰胺衍生物; 然后将衍生物去保护以转化为α-氨基-α-羟基甲酰胺衍生物; 并使用质子性溶剂使衍生物结晶，得到结晶。通过该工艺可以在工业规模上稳定地生产高纯度和β-氨基-α-羟基甲酰胺衍生物。

8. 发明授权

US07973176B2 Process for production of aralkyloxypyrrolidine derivative 有权
标题翻译：制备芳烷氧基吡咯烷衍生物的方法
公开(公告)号：US07973176B2
公开(公告)日：2011-07-05
申请号：US11990766
申请日：2006-08-22
申请人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
发明人： Toshihiro Takeda , Masatoshi Ohnuki , Narumi Kishimoto
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译：本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。

9. 发明授权

US07807426B2 Processes for producing optically active 1-substituted 2-methylpyrrolidine 失效
标题翻译：光学活性1-取代2-甲基吡咯烷的制备方法
公开(公告)号：US07807426B2
公开(公告)日：2010-10-05
申请号：US10586337
申请日：2005-01-19
申请人： Akira Nishiyama , Naoaki Taoka , Narumi Kishimoto , Nobuo Nagashima
发明人： Akira Nishiyama , Naoaki Taoka , Narumi Kishimoto , Nobuo Nagashima
IPC分类号： C12P7/18 , C12P7/00
CPC分类号： C12P17/10 , C07C303/28 , C12P7/18 , C12P11/00 , C07C309/66
摘要： The present invention relates to a process for producing an optically active 1,4-pentanediol by asymmetrically reducing 5-hydroxy-2-pentanone, which is easily available at low cost. The present invention also relates to a process for producing an optically active 1-substituted 2-methylpyrrolidine including sulfonylating the optically active 1,4-pentanediol to convert it to an optically active sulfonate compound, and reacting the compound with an amine. According to the processes of the present invention, an optically active 1,4-pentanediol and an optically active 1-substituted 2-methylpyrrolidine, which are useful as an intermediate for medicines and an intermediate for agricultural chemicals, can be simply produced from an inexpensive starting material.
摘要翻译：本发明涉及通过不对称地还原5-羟基-2-戊酮来制备光学活性的1,4-戊二醇的方法，该方法容易以低成本获得。本发明还涉及一种光学活性1-取代的2-甲基吡咯烷的制备方法，其包括使光学活性的1,4-戊二醇磺酰化以将其转化成光学活性的磺酸盐化合物，并使该化合物与胺反应。根据本发明的方法，用作药物中间体和农药中间体的光学活性的1,4-丁二醇和光学活性的1-取代的2-甲基吡咯烷可以简便地从廉价的起始材料

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