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    NOVEL IMIDAZOLIDINONE DERIVATIVE, METHOD OF PRODUCING THE SAME AND METHOD OF PRODUCING OPTICALLY ACTIVE AMINO ACID
    3.
    发明公开
    NOVEL IMIDAZOLIDINONE DERIVATIVE, METHOD OF PRODUCING THE SAME AND METHOD OF PRODUCING OPTICALLY ACTIVE AMINO ACID 有权
    NEW咪唑啉酮衍生物，的制造方法及其制造方法的光学活性氨基

    公开(公告)号：EP2050738A1

    公开(公告)日：2009-04-22

    申请号：EP07743261.5

    申请日：2007-05-14

    申请人： Kaneka Corporation

    发明人： SAKA, Yasuhiro ,  FUJII, Akio ,  OKURO, Kazumi ,  MITSUDA, Masaru

    IPC分类号： C07D233/32 ,  C07C227/22 ,  C07C229/08 ,  C07C229/22 ,  C07C229/36 ,  C07B61/00

    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 cromatography.

    摘要翻译： 本发明的目的是提供衍生的光学活性咪唑烷酮衍生物的广泛可用于光学活性的氨基酸，从而产生容易衍生物的方法，和在氨基酸旋光简便地制造使用的方法合成。 目的可以通过使用一种新颖的光学由通式（3）等为代表的活性咪唑烷酮衍生物在光学活性的氨基酸生产来实现。 。根据本发明的方法中，衍生物的光学活性咪唑烷酮衍生物可以通过优先结晶从咪唑啉酮的异构体的混合物得到。 因此，在光学活性的氨基酸可被立体选择性地容易和没有用于所述的常规方法需要麻烦的程序生产，谋求作为从光学活性的氨基酸非对映体的拆分，合成，并在通过硅胶柱cromatography异构体的分辨率。

    NOVEL PYRIMIDINE DERIVATIVE AND METHOD FOR PRODUCING HMG-CoA REDUCTASE INHIBITOR INTERMEDIATE
    6.
    发明公开
    NOVEL PYRIMIDINE DERIVATIVE AND METHOD FOR PRODUCING HMG-CoA REDUCTASE INHIBITOR INTERMEDIATE 有权
    消除PYRIMIDINDERIVAT UND VERFAHREN ZUR HERSTELLUNG EINES ZWISCHENPRODUKTS EINES HMG-COA-REDUKTASEINHIBITORS

    公开(公告)号：EP2351762A1

    公开(公告)日：2011-08-03

    申请号：EP09821993.4

    申请日：2009-10-19

    申请人： Kaneka Corporation

    发明人： SAKA, Yasuhiro ,  NISHIYAMA, Akira

    IPC分类号： C07F9/6512 ,  C07D405/06

    CPC分类号： C07F9/65122 ,  C07D405/06

    摘要： The problem to be solved of the present application is to provide a method for producing a novel pyrimidine derivative from an inexpensive compound which is industry-available with ease, and a method for producing an important intermediate of an HMG-CoA reductase inhibitor. The problem can be solved by, for example, reacting the compound (1) with the compound represented by (OR 1 ) 3P to obtain the phosphonate ester (3) and reacting the phosphonate ester (3) with the compound (4) in the presence of a base to obtain an HMG-CoA reductase inhibitor intermediate (5).

    摘要翻译： 本申请要解决的问题是提供从便宜的化合物制备新颖的嘧啶衍生物的方法，其易于工业可用，以及生产HMG-CoA还原酶抑制剂的重要中间体的方法。 该问题可以通过例如使化合物（1）与由（OR 1）3 P表示的化合物反应得到膦酸酯（3）并使膦酸酯（3）与化合物（4）在 存在碱以获得HMG-CoA还原酶抑制剂中间体（5）。

    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 有权
    方法环化的光学活性4-氨基-2-丁HALOGEN

    公开(公告)号：EP1253140B1

    公开(公告)日：2005-01-12

    申请号：EP01902737.4

    申请日：2001-02-02

    申请人： KANEKA CORPORATION

    发明人： SAKA, Yasuhiro ,  HONDA, Tatsuya ,  NAGASHIMA, Nobuo

    IPC分类号： C07D205/04

    CPC分类号： C07D205/04

    摘要： A process for preparing optically active azetidine -2-carboxylic acid efficiently, easily, simply, and industrially advantageously by cyclizing an optically active 4-amino- 2-halogenobutyric acid in an optical yield of as high as 90 % or above. Specifically, a process for preparing optically active azetidine-2-carboxylic acid of formula (2) (wherein * represents an asymmetric carbon atom) by cyclizing an optically active 4-amino-2-halogenobutyric acid of the general formula (1) (wherein X is halogeno and * represents an asymmetric carbon atom) in the presence of an alkaline earth metal oxide, an alkaline earth metal hydroxide except barium hydroxide, or an organic amine.

    PROCESS FOR CYCLIZING OPTICALLY ACTIVE 4-AMINO-2-HALOGENOBUTYRIC ACIDS
    8.
    发明公开
    PROCESS FOR CYCLIZING OPTICALLY ACTIVE 4-AMINO-2-HALOGENOBUTYRIC ACIDS 有权
    VERFAHREN ZUR ZYKLISIERUNG VON OPTISCH AKTIVEN 4-AMINO-2-HALOGENBUTTERSÄUREN

    公开(公告)号：EP1253140A1

    公开(公告)日：2002-10-30

    申请号：EP01902737.4

    申请日：2001-02-02

    申请人： KANEKA CORPORATION

    发明人： SAKA, Yasuhiro ,  HONDA, Tatsuya ,  NAGASHIMA, Nobuo

    IPC分类号： C07D205/04

    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，其包括将光学活性4-氨基-2-卤代丁酸以高达90％的光学收率环化，或 更多。 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，其包括使通式（1）的光学活性4-氨基-2-卤代丁酸环化， 1），其中X表示卤素原子，*表示不对称碳原子，在碱土金属的氧化物，除钡以外的碱土金属的氢氧化物或有机胺的存在下进行。

    PROCESS FOR THE PREPARATION OF 3-HYDROXYTETRAHYDROFURAN
    9.
    发明公开
    PROCESS FOR THE PREPARATION OF 3-HYDROXYTETRAHYDROFURAN 有权
    制备3-羟基四氢呋喃的方法

    公开(公告)号：EP1088820A1

    公开(公告)日：2001-04-04

    申请号：EP00915524.3

    申请日：2000-04-14

    申请人： KANEKA CORPORATION

    发明人： KINOSHITA, Koichi ,  MOROSHIMA, Tadashi ,  YANAGIDA, Yoshifumi ,  NAGASHIMA, Nobuo ,  SAKA, Yasuhiro ,  HONDA, Tatsuya ,  FUSE, Yoshihide ,  UEDA, Yasuyoshi

    IPC分类号： C07D307/20 ,  C07C29/147 ,  C07C31/42

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

    摘要： An industrially advantageous process for preparing high-purity 3-hydroxytetrahydrofuran easily and simply, which comprises converting a 4-halo-3-hydroxybutyric acid ester into a 4-halo-1,3-butanediol by reducing the ester with a boron hydride compound and/or an aluminum hydride compound in an organic solvent incompatible with water and treating the obtained reaction mixture with an acid and water, recovering an aqueous solution containing the diol, conducting the cyclization of the diol in this aqueous solution, extracting the resulting solution with an organic solvent incompatible with water, and isolating 3-hydroxytetrahydrofuran from the extract through concentration and/or distillation.

    摘要翻译： 一种容易且简单地制备高纯度3-羟基四氢呋喃的工业上有利的方法，该方法包括通过用氢化硼化合物还原酯将4-卤代-3-羟基丁酸酯转化成4-卤代-1,3-丁二醇和 /或氢化铝化合物溶于与水不相容的有机溶剂中，并用酸和水处理得到的反应混合物，回收含有二醇的水溶液，在该水溶液中进行二醇的环化，将所得溶液用 与水不相容的有机溶剂，并通过浓缩和/或蒸馏从提取物中分离3-羟基四氢呋喃。