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公开(公告)号：US08084611B2
公开(公告)日：2011-12-27
申请号：US12295618
申请日：2007-03-29
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
IPC分类号： C07D215/38
CPC分类号： C07D215/42 , C07D215/233
摘要： The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
摘要翻译： 本发明提供一种可用于治疗和/或预防动脉硬化疾病，血脂异常等疾病的光学活性四氢喹啉衍生物的方法及其合成中间体的制备方法。 具体地说，（2R，4S）-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐在不使用光学拆分的情况下以较少的步骤制备，并且光学活性的四氢喹啉衍生物 由胺化合物得到。
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公开(公告)号：US20090292125A1
公开(公告)日：2009-11-26
申请号：US12295618
申请日：2007-03-29
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
IPC分类号： C07D215/38
CPC分类号： C07D215/42 , C07D215/233
摘要： The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
摘要翻译： 本发明提供一种可用于治疗和/或预防动脉硬化疾病，血脂异常等疾病的光学活性四氢喹啉衍生物的方法及其合成中间体的制备方法。 具体地说，（2R，4S）-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐在不使用光学拆分的情况下以较少的步骤制备，并且光学活性的四氢喹啉衍生物 由胺化合物得到。
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3.发明授权公开(公告)号：US08754221B2
公开(公告)日：2014-06-17
申请号：US13747376
申请日：2013-01-22
IPC分类号： C07D215/233 , C07D401/04
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译： 本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示不对称碳原子]，其包含 在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。
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公开(公告)号：US08471028B2
公开(公告)日：2013-06-25
申请号：US13087588
申请日：2011-04-15
IPC分类号： C07D401/04
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译： 本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示不对称碳原子]，其包含 在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。
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5.发明申请公开(公告)号：US20130237708A1
公开(公告)日：2013-09-12
申请号：US13747376
申请日：2013-01-22
IPC分类号： C07D215/233 , C07D401/04
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译： 本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示不对称碳原子]，其包含 在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。
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6.发明申请公开(公告)号：US20100152451A1
公开(公告)日：2010-06-17
申请号：US12089170
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
IPC分类号： C07D215/233
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译： 本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示不对称碳原子]，其包含 在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。
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7.发明授权Method of enzymatic optical resolution of racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline 有权外消旋4-羟基-1,2,3,4-四氢喹啉的酶学光学拆分方法公开(公告)号：US07972836B2
公开(公告)日：2011-07-05
申请号：US12083014
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
发明人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
CPC分类号： C07D215/233 , C07B51/00 , C07B53/00 , C07D215/06 , C07D215/08 , C07D401/04 , C12P17/12 , C12P41/005 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active 4-hydroxy-1,2,3,4-tetrahydroquinoline compound [I], which comprises the steps of: treating a racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline compound represented by general formula [I]: [wherein R1 represents a hydrogen atom or a protecting group for amino group.] with an enzyme having an ability of selectively or preferentially acylating one enantiomer of the racemic compound [I] in the presence of an acyl donor; and if necessary, subjecting the reaction product to solvolysis.
摘要翻译： 本发明涉及一种制备光学活性4-羟基-1,2,3,4-四氢喹啉化合物[I]的方法，其包括以下步骤：将外消旋的4-羟基-1,2,3,4 通式[I]表示的四氢喹啉化合物：[其中R1表示氢原子或氨基保护基]与具有选择性或优先酰化外消旋化合物[I]的一种对映异构体的能力的酶在存在下 的酰基供体; 并且如果需要，使反应产物溶解。
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8.发明申请Method for Preparing Optically Active 4-Hydroxy-1,2,3,4-Tetrahydroquinoline Compound 有权光学活性4-羟基-1,2,3,4-四氢喹啉化合物的制备方法公开(公告)号：US20090269821A1
公开(公告)日：2009-10-29
申请号：US12083014
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
发明人： Masaki Okamoto , Akira Sakuragi , Muneki Kishida , Yoshikazu Mori
CPC分类号： C07D215/233 , C07B51/00 , C07B53/00 , C07D215/06 , C07D215/08 , C07D401/04 , C12P17/12 , C12P41/005 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active 4-hydroxy-1,2,3,4-tetrahydroquinoline compound [I], which comprises the steps of:treating a racemic 4-hydroxy-1,2,3,4-tetrahydroquinoline compound represented by general formula [I]: [wherein R1 represents a hydrogen atom or a protecting group for amino group.] with an enzyme having an ability of selectively or preferentially acylating one enantiomer of the racemic compound [I] in the presence of an acyl donor; and if necessary, subjecting the reaction product to solvolysis.
摘要翻译： 本发明涉及一种制备光学活性4-羟基-1,2,3,4-四氢喹啉化合物[I]的方法，其包括以下步骤：将外消旋的4-羟基-1,2,3,4 通式[I]表示的四氢喹啉化合物：[其中R1表示氢原子或氨基保护基]与具有选择性或优先酰化外消旋化合物[I]的一种对映异构体的能力的酶在存在下 的酰基供体; 并且如果需要，使反应产物溶解。
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9.发明授权公开(公告)号：US07989627B2
公开(公告)日：2011-08-02
申请号：US12089170
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
IPC分类号： C07D215/00 , C07D215/233
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an astymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.]to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译： 本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示非对称碳原子]，其包含 在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。
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公开(公告)号：US20100248541A1
公开(公告)日：2010-09-30
申请号：US12725634
申请日：2010-03-17
申请人： Masaki Okamoto
发明人： Masaki Okamoto
IPC分类号： H01R13/648
CPC分类号： H01R13/648 , H01R13/504 , H01R43/24
摘要： A shield connector (C) includes a tubular metallic shield shell (30) integrally attached to the outer circumferential surface of a housing (10) made of resin by insert molding. The shield shell (30) is formed with a cut (32) extending between opposite ends in a longitudinal direction, and a pair of opening preventing pieces (34A, 34B) which extend radially inward or outward, circumferentially face each other and can come into contact with each other when edges (33A, 33B) at the opposite sides of the cut (32) are displaced in directions away from each other are provided on the opposite edges (33A, 33B) of the shield shell 30 facing each other with the cut (32) therebetween.
摘要翻译： 屏蔽连接器（C）包括通过插入成型一体地附接到由树脂制成的壳体（10）的外周表面的管状金属屏蔽壳（30）。 屏蔽壳30形成有在长度方向的相对端之间延伸的切口（32），并且一对径向向内或向外延伸的开口防止件（34A，34B）彼此周向地面对，并且可以进入 在屏蔽壳30的彼此面对的相对边缘（33A，33B）上设置有在切割部（32）的相对侧上的边缘（33A，33B）彼此偏离的方向上彼此相对的方式彼此接触， 在它们之间切割（32）。
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