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    Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative
    1.
    发明授权
    Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative 失效
    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。

    Method for producing optically-active 2-piperazinecarboxylic acid derivatives
    2.
    发明授权
    Method for producing optically-active 2-piperazinecarboxylic acid derivatives 有权
    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。

    Processes for the recovery of optically active diacyltartaric acids
    4.
    发明授权
    Processes for the recovery of optically active diacyltartaric acids 有权
    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。

    Processes for the recovery of optically active diacyltartatic acids
    5.
    发明申请
    Processes for the recovery of optically active diacyltartatic acids 有权
    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。

    Process for producing oxycarbonyl-substituted piperazine derivative
    6.
    发明授权
    Process for producing oxycarbonyl-substituted piperazine derivative 有权
    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。

    Method of producing pyrrolidine derivatives
    8.
    发明授权
    Method of producing pyrrolidine derivatives 有权
    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。

    Methods for making optically active 3-aminopyrrolidine-2,5-dione derivative and optically active 3-aminopyrrolidine derivative
    9.
    发明授权
    Methods for making optically active 3-aminopyrrolidine-2,5-dione derivative and optically active 3-aminopyrrolidine derivative 失效
    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。