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1. 发明申请

US20060270847A1 Process for producing nitrogenous heterocyclic compound 审中-公开
标题翻译：含氮杂环化合物的制备方法
公开(公告)号：US20060270847A1
公开(公告)日：2006-11-30
申请号：US10562405
申请日：2004-06-22
申请人： Seiji Morii , Takae Ono , Haruyo Sato
发明人： Seiji Morii , Takae Ono , Haruyo Sato
IPC分类号： C07D223/12 , C07D211/26
CPC分类号： C07D207/12 , B01J23/44
摘要： A nitrogenous heterocyclic compound such as 3-aminopyrrolidine derivative is produced by hydrogenolysis of an N-substituted nitrogenous heterocyclic compound with normal pressure hydrogen in a water-based solvent in presence of a catalyst. In the case an optically active 1-substituted-3-aminopyrrrolidine derivative is used as a raw material, an optically active 3-aminopyrrolidine derivative can be obtained as a product practically without racemination.
摘要翻译：通过在催化剂存在下，在水系溶剂中，用常压氢氢解N-取代的含氮杂环化合物，制得3-氨基吡咯烷衍生物等含氮杂环化合物。在使用旋光性1-取代-3-氨基吡咯烷衍生物作为原料的情况下，可以获得光学活性的3-氨基吡咯烷衍生物作为产物，实际上没有外消旋化。

2. 发明授权

US06348600B1 Methods for making optically active 3-aminopyrrolidine-2,5-dione derivative and optically active 3-aminopyrrolidine derivative 失效
标题翻译：制备光学活性3-氨基吡咯烷-2,5-二酮衍生物和光学活性3-氨基吡咯烷衍生物的方法
公开(公告)号：US06348600B1
公开(公告)日：2002-02-19
申请号：US09788944
申请日：2001-02-20
申请人： Takae Ono , Haruyo Sato
发明人： Takae Ono , Haruyo Sato
IPC分类号： C07D20750
CPC分类号： C07D207/416 , C07D207/14
摘要： A method for making an optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3) includes cyclizing an optically active asparagine ester derivative represented by the formula (1) or (2), or an acid salt thereof. A method for making an optically active 3-aminopyrrolidine derivative represented by the formula (9) includes reducing the optically active 3-aminopyrrolidine-2,5-dione derivative represented by the formula (3). A method for making an optically active 3-aminopyrrolidine derivative includes hydrogenolyzing the optically active 3-aminopyrrolidine derivative represented by the formula (9).
摘要翻译：制备由式（3）表示的光学活性3-氨基吡咯烷-2,5-二酮衍生物的方法包括使由式（1）或（2）表示的光学活性天冬酰胺酯衍生物或其酸式盐进行环化。制备由式（9）表示的光学活性3-氨基吡咯烷衍生物的方法包括还原由式（3）表示的光学活性3-氨基吡咯烷-2,5-二酮衍生物。制备光学活性3-氨基吡咯烷衍生物的方法包括使由式（9）表示的光学活性3-氨基吡咯烷衍生物氢解。

3. 发明授权

US07358384B2 Processes for the recovery of optically active diacyltartaric acids 有权
标题翻译：回收光学活性二酰基酒石酸的方法
公开(公告)号：US07358384B2
公开(公告)日：2008-04-15
申请号：US10542498
申请日：2003-12-22
申请人： Seiji Morii , Toshihiro Fujino , Haruyo Sato
发明人： Seiji Morii , Toshihiro Fujino , Haruyo Sato
IPC分类号： C07C69/76 , C07C69/66 , C07C51/42 , C07C59/255
CPC分类号： C07C67/52 , C07B2200/07 , Y02P20/582 , C07C69/76
摘要： When a salt of an amine and an optically active diacyltartaric acid, or a diastereomer salt of an optically active amine and an optically active diacyltartaric acid, obtained by optically resolving a racemic amine using the optically active diacyltartaric acid, is salt-exchanged with an acid aqueous solution, the optically active diacyltartaric acid is added in the acid aqueous solution beforehand.Furthermore, a raw material containing a racemic amine and an optically active diacyltartaric acid is optically resolved, and the diastereomer salt of the optically active amine and the optically active diacyltartaric acid respectively of one isomer type, is separated. The obtained diastereomer salt is dissociated using an acid aqueous solution containing the optically active diacyltartaric acid, for recovering the optically active diacyltartaric acid, and the obtained optically active diacyltartaric acid is recycled into an optical resolution step as a raw material of the optical resolution step.
摘要翻译：当通过光学拆分外消旋胺使用光学活性的二酰基酒石酸获得的胺和光学活性二酰基酒石酸盐或光学活性胺和光学活性二酰基酒石酸的非对映体盐与酸盐交换时，水溶液中，将光学活性的二酰基酒石酸预先加入到酸性水溶液中。此外，含有外消旋胺和光学活性二酰基酒石酸的原料被光学拆分，分离出一种异构体类型的光学活性胺和光学活性二酰基酒石的非对映异构体盐。使用含有光学活性二酰基酒石酸的酸性水溶液使得到的非对映异构体盐解离，回收光学活性的二酰基酒石酸，将得到的光学活性二酰基酒石再循环至作为光学拆分工序的原料的光学拆分工序。

4. 发明申请

US20060058546A1 Processes for the recovery of optically active diacyltartatic acids 有权
标题翻译：回收光学活性二酰基鞣酸的方法
公开(公告)号：US20060058546A1
公开(公告)日：2006-03-16
申请号：US10542498
申请日：2003-12-22
申请人： Seiji Morii , Toshihiro Fujino , Haruyo Sato
发明人： Seiji Morii , Toshihiro Fujino , Haruyo Sato
IPC分类号： C07C69/86 , C07C69/66
CPC分类号： C07C67/52 , C07B2200/07 , Y02P20/582 , C07C69/76
摘要： When a salt of an amine and an optically active diacyltartaric acid, or a diastereomer salt of an optically active amine and an optically active diacyltartaric acid, obtained by optically resolving a racemic amine using the optically active diacyltartaric acid, is salt-exchanged with an acid aqueous solution, the optically active diacyltartaric acid is added in the acid aqueous solution beforehand. Furthermore, a raw material containing a racemic amine and an optically active diacyltartaric acid is optically resolved, and the diastereomer salt of the optically active amine and the optically active diacyltartaric acid respectively of one isomer type, is separated. The obtained diastereomer salt is dissociated using an acid aqueous solution containing the optically active diacyltartaric acid, for recovering the optically active diacyltartaric acid, and the obtained optically active diacyltartaric acid is recycled into an optical resolution step as a raw material of the optical resolution step.
摘要翻译：当通过光学拆分外消旋胺使用光学活性的二酰基酒石酸获得的胺和光学活性二酰基酒石酸盐或光学活性胺和光学活性二酰基酒石酸的非对映体盐与酸盐交换时，水溶液中，将光学活性的二酰基酒石酸预先加入到酸性水溶液中。此外，含有外消旋胺和光学活性二酰基酒石酸的原料被光学拆分，分离出一种异构体类型的光学活性胺和光学活性二酰基酒石的非对映异构体盐。使用含有光学活性二酰基酒石酸的酸性水溶液使得到的非对映异构体盐解离，回收光学活性的二酰基酒石酸，将得到的光学活性二酰基酒石再循环至作为光学拆分工序的原料的光学拆分工序。

5. 发明授权

US07569690B2 Process for producing oxycarbonyl-substituted piperazine derivative 有权
标题翻译：氧羰基取代的哌嗪衍生物的制备方法
公开(公告)号：US07569690B2
公开(公告)日：2009-08-04
申请号：US10524517
申请日：2003-09-02
申请人： Masao Morimoto , Haruyo Sato
发明人： Masao Morimoto , Haruyo Sato
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07D295/205
摘要： If an organic solvent with a water content of 15% or less is used when an oxycarbonyl-substituted piperazine derivative is produced from a piperazine derivative, the piperazine derivative can be oxycarbonylated.
摘要翻译：当由哌嗪衍生物生成氧羰基取代的哌嗪衍生物时，如果使用含水率为15％以下的有机溶剂，则可以将哌嗪衍生物进行氧羰基化。

6. 发明授权

US06962998B2 Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative 失效
标题翻译：用于制备外消旋哌啶衍生物和用于制备光学活性哌啶衍生物的方法
公开(公告)号：US06962998B2
公开(公告)日：2005-11-08
申请号：US10296772
申请日：2001-06-04
申请人： Toshihiro Fujino , Haruyo Sato
发明人： Toshihiro Fujino , Haruyo Sato
IPC分类号： C07D211/24 , C07D211/10 , C07D211/14
CPC分类号： C07D211/24 , Y02P20/582
摘要： Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a method for producing optically-active piperidine derivatives or their acid salts by optically resolving the racemic piperidine derivatives obtained in the former method.
摘要翻译：公开了在还原催化剂存在下，在氢气氛中加工光学活性哌啶衍生物来制备外消旋哌啶衍生物的方法; 以及通过光学拆分前述方法得到的外消旋哌啶衍生物来制造光学活性哌啶衍生物或其酸式盐的方法。

7. 发明授权

US06706916B1 Optically active amino acid derivatives and processes for the preparation of the same 失效
标题翻译：光学活性氨基酸衍生物及其制备方法
公开(公告)号：US06706916B1
公开(公告)日：2004-03-16
申请号：US09913822
申请日：2001-08-17
申请人： Haruyo Sato , Takae Ohno , Shiho Iwata
发明人： Haruyo Sato , Takae Ohno , Shiho Iwata
IPC分类号： C07C30900
CPC分类号： C07C227/32 , C07B2200/07 , C07C227/18 , C07C231/18 , C07C229/08 , C07C229/24 , C07C229/26 , C07C233/47 , C07C235/12
摘要： In producing optically-active amino acid benzyl esters by reacting optically-active amino acids with benzyl alcohols, hydrazines are present in the reaction system, or the compounds are reacted in the absence of oxygen, or the compounds are reacted in the absence of oxygen while hydrazines are present in the reaction system. The processes are simple and give optically-active amino acid benzyl esters of high optical purity.
摘要翻译：在光学活性氨基酸与苄醇反应制备光学活性氨基酸苄基酯时，肼在反应体系中存在，或者化合物在不存在氧的情况下反应，或者化合物在不存在氧的情况下反应，而肼存在于反应体系中。该方法简单，得到光学纯度高的光学活性氨基酸苄基酯。

8. 发明授权

US5952503A Method for producing optically-active 2-piperazinecarboxylic acid derivatives 有权
标题翻译：光学活性2-哌嗪羧酸衍生物的制备方法
公开(公告)号：US5952503A
公开(公告)日：1999-09-14
申请号：US125840
申请日：1998-08-26
申请人： Toshihiro Fujino , Haruyo Sato
发明人： Toshihiro Fujino , Haruyo Sato
IPC分类号： C07D241/04 , C07B57/00 , C07C233/46 , C07C233/83 , C07C271/22 , C07C311/04 , C07C311/06 , C07C311/08
CPC分类号： C07D241/04
摘要： Optically-active 2-piperazinecarboxylic acid derivatives are produced through diastereomer salt resolution using optically-active acidic amino acid derivative as the resolving reagent. In this method, the recovery of the resolving reagent used is high, and the production efficiency to produce the optically-active products is high. As the optically-active acidic amino acid derivatives, usable are optically-active, N-acylated acidic amino acid derivatives and optically-active, N-sulfonylated acidic amino acid derivatives.
摘要翻译： PCT No.PCT / JP96 / 03864 Sec。 371日期：1998年8月26日 102（e）1998年8月26日PCT 1996年12月27日PCT PCT。公开号WO98 / 29398 日期1998年7月9日光学活性的2-哌嗪羧酸衍生物是通过使用光学活性的酸性氨基酸衍生物作为拆分试剂的非对映异构体盐分解制备的。在该方法中，所使用的拆分试剂的回收率高，生产光学活性物质的生产效率高。作为光学活性的酸性氨基酸衍生物，可以使用光学活性的N-酰化酸性氨基酸衍生物和光学活性的N-磺酰化酸性氨基酸衍生物。

9. 发明授权

US06479668B1 Method of producing pyrrolidine derivatives 有权
标题翻译：制备吡咯烷衍生物的方法
公开(公告)号：US06479668B1
公开(公告)日：2002-11-12
申请号：US09558798
申请日：2000-04-26
申请人： Hideo Muraoka , Haruyo Sato
发明人： Hideo Muraoka , Haruyo Sato
IPC分类号： C07D20712
CPC分类号： C07D491/04 , C07D207/12 , C07D207/14
摘要： A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.
摘要翻译：公开了一种通过在至少一种酸的存在下用至少一种过氧化物氧化3-吡咯啉来制备吡咯烷衍生物如3,4-环氧吡啶，3-吡咯烷醇等的方法。通过从顺式-2-丁烯-1,4-二醇衍生顺式-2-丁烯化合物并在顺式-2-丁烯衍生物与至少一种伯胺之间进行环化来制备3-吡咯啉。该方法可以作为一锅合成进行，并且可以作为连续反应进行。

10. 发明授权

US5451687A Process for producing O,O'-diacyltartaric anhydride and process for producing O,O'-diacyltartaric acid 失效
标题翻译：制备O，O-二酰基酒石酸酐的方法和制备O，O-二酰基酒石酸的方法
公开(公告)号：US5451687A
公开(公告)日：1995-09-19
申请号：US158424
申请日：1993-11-29
申请人： Haruyo Sato , Sakie Nakai , Toshihiro Fujino
发明人： Haruyo Sato , Sakie Nakai , Toshihiro Fujino
IPC分类号： C07D307/56 , C07C67/52 , C07C69/70 , C07C69/76 , C07C69/78 , C07D307/34 , C07C59/255
CPC分类号： C07C69/78 , C07C67/52 , C07C69/70 , C07C69/76
摘要： An industrial process for producing O,O'-diacyltartaric anhydride with high purity and high efficiency is disclosed. According to the process of the invention, a carboxylic acid of the formula (I):R.sup.1 COOH (I)(wherein R.sup.1 represents C.sub.1 -C.sub.4 alkyl group; phenyl group; or phenyl group substituted with 1-5 C.sub.1 -C.sub.4 alkyl groups or with 1-5 halogen atoms) is reacted with tartaric acid in the presence of a chlorinating agent.
摘要翻译：公开了用于生产高纯度和高效率的O，O-二酰基酒石酸酐的工业方法。根据本发明的方法，式（I）的羧酸：R 1 COOH（I）（其中R 1表示C 1 -C 4烷基;苯基;或被1-5个C 1 -C 4烷基取代的苯基或与 1-5个卤素原子）与酒石酸在氯化剂存在下反应。

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