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    Process for the preparation of 3-hydroxytetrahydrofuran
    4.
    发明授权
    Process for the preparation of 3-hydroxytetrahydrofuran 失效
    3-羟基四氢呋喃的制备方法

    公开(公告)号：US06359155B1

    公开(公告)日：2002-03-19

    申请号：US09719686

    申请日：2001-02-15

    申请人： Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Nobuo Nagashima ,  Yasuhiro Saka ,  Tatsuya Honda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    发明人： Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Nobuo Nagashima ,  Yasuhiro Saka ,  Tatsuya Honda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    IPC分类号： C07D30720

    CPC分类号： C07C29/147 ,  C07B2200/07 ,  C07D307/20 ,  Y02P20/55 ,  C07C31/42

    摘要： An industrial advantage process for producing high-purity 3-hydroxytetrahydrofuran easily and simply, which comprises reducing a 4-halo-3-hydroxybutyric acid ester (1) with a boron hydride compound and/or an aluminum hydride compound as a reducing agent in an organic solvent immiscible with water; treating the reaction mixture with an acid and water to thereby effect conversion to the corresponding 4-halo-1,3-butanediol and at the same time giving an aqueous solution containing said compound; carrying out the cyclization reaction of the 4-halo-1,3-butanediol in said aqueous solution; extracting the resulting 3-hydroxytetrahydrofuran from the 3-hydroxytetrahydrofuran-containing aqueous solution using an organic solvent immiscible with water; and isolating the 3-hydroxytetrahydrofuran by concentration and/or distillation of the solution obtained.

    摘要翻译： 用于容易且简单地生产高纯度3-羟基四氢呋喃的工业优势方法，其包括用硼氢化合物和/或氢化铝化合物作为还原剂还原4-卤代-3-羟基丁酸酯（1） 与水不混溶的有机溶剂;用酸和水处理反应混合物，从而转化为相应的4-卤代-1,3-丁二醇，同时得到含有所述化合物的水溶液;进行环化反应 所述水溶液中的4-卤代-1,3-丁二醇;使用与水不混溶的有机溶剂从含3-羟基四氢呋喃的水溶液中萃取所得3-羟基四氢呋喃; 通过所得溶液的浓缩和/或蒸馏来使3-羟基四氢呋喃分离。

    NOVEL IMIDAZOLIDINONE DERIVATIVE, METHOD OF PRODUCING THE SAME AND METHOD OF PRODUCING OPTICALLY ACTIVE AMINO ACID
    5.
    发明申请
    NOVEL IMIDAZOLIDINONE DERIVATIVE, METHOD OF PRODUCING THE SAME AND METHOD OF PRODUCING OPTICALLY ACTIVE AMINO ACID 有权
    新型咪唑烷酮衍生物及其制备方法和生产光学活性氨基酸的方法

    公开(公告)号：US20090209768A1

    公开(公告)日：2009-08-20

    申请号：US12309729

    申请日：2007-05-14

    申请人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    发明人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    IPC分类号： C07D233/32 ,  C07C229/36 ,  C07C229/08 ,  C07C229/22

    CPC分类号： C07D233/32 ,  C07C227/22 ,  C07C231/10 ,  C07C229/14 ,  C07C229/22 ,  C07C229/36 ,  C07C237/06

    摘要： The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

    摘要翻译： 本发明的目的是提供广泛用于合成光学活性氨基酸的光学活性咪唑啉酮衍生物，易于制备衍生物的方法，以及使用该衍生物容易地制备光学活性氨基酸的方法。 可以通过使用由通式（3）等表示的新的光学活性咪唑烷酮衍生物制造光学活性氨基酸来实现。 根据本发明的方法，可以通过从咪唑烷酮衍生物的异构体的混合物中优先结晶获得光学活性咪唑烷酮衍生物。 因此，光学活性氨基酸可以容易地和立体选择性地产生，而不需要常规方法所需的繁琐程序，例如拆分非对映异构体，由光学活性氨基酸的合成和通过硅胶柱色谱法拆分异构体。

    Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid
    6.
    发明授权
    Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid 有权
    咪唑啉酮衍生物，其制备方法和制备光学活性氨基酸的方法

    公开(公告)号：US07947722B2

    公开(公告)日：2011-05-24

    申请号：US12309729

    申请日：2007-05-14

    申请人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    发明人： Yasuhiro Saka ,  Akio Fujii ,  Kazumi Okuro ,  Masaru Mitsuda

    IPC分类号： A61K31/4166 ,  C07D233/32

    CPC分类号： C07D233/32 ,  C07C227/22 ,  C07C231/10 ,  C07C229/14 ,  C07C229/22 ,  C07C229/36 ,  C07C237/06

    摘要： The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.

    摘要翻译： 本发明的目的是提供广泛用于合成光学活性氨基酸的光学活性咪唑啉酮衍生物，易于制备衍生物的方法，以及通过使用该衍生物容易地制备光学活性氨基酸的方法。 可以通过使用由通式（3）等表示的新的光学活性咪唑烷酮衍生物制造光学活性氨基酸来实现。 根据本发明的方法，可以通过从咪唑烷酮衍生物的异构体的混合物中优先结晶获得光学活性咪唑烷酮衍生物。 因此，光学活性氨基酸可以容易地和立体选择性地产生，而不需要常规方法所需的繁琐程序，例如拆分非对映异构体，由光学活性氨基酸的合成和通过硅胶柱色谱法拆分异构体。

    Process for cyclizing optically active 4-amino-2-halogenobutyric acids
    7.
    发明授权
    Process for cyclizing optically active 4-amino-2-halogenobutyric acids 失效
    环化光学活性4-氨基-2-卤代丁酸的方法

    公开(公告)号：US06747161B2

    公开(公告)日：2004-06-08

    申请号：US10182649

    申请日：2002-11-01

    申请人： Yasuhiro Saka ,  Tatsuya Honda ,  Nobuo Nagashima

    发明人： Yasuhiro Saka ,  Tatsuya Honda ,  Nobuo Nagashima

    IPC分类号： C07D20500

    CPC分类号： C07D205/04

    摘要： The invention provides a process for producing optically active azetidine-2-carboxylic acid with good efficiency, expedience, and commercial advantage, which comprises cyclizing an optically active 4-amino-2-halogenobutyric acid in an optical yield of as high as 90% or more. It is a process for producing optically active azetidine-2-carboxylic acid of the general formula (2), in which * denotes an asymmetric carbon atom, which comprises cyclizing an optically active 4-amino-2-halogenobutyric acid of the general formula (1), in which X represents a halogen atom and * denotes an asymmetric carbon atom, in the presence of an oxide of an alkaline earth metal, a hydroxide of an alkaline earth metal excepting barium, or an organic amine.

    摘要翻译： 本发明提供了一种以高效率，便利和商业优点制备光学活性氮杂环丁烷-2-羧酸的方法，该方法包括使光学活性4-氨基-2-卤代丁酸以高达90％的光学收率环化;或 它是制备通式（2）的光学活性氮杂环丁烷-2-羧酸的方法，其中*表示不对称碳原子，其包括使一般的光学活性4-氨基-2-卤代丁酸环化 在碱土金属的氧化物，除了钡以外的碱土金属的氢氧化物或有机胺的存在下，式（1）中X表示卤素原子，*表示不对称碳原子。