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    Method for producing an optically active β-amino acid
    1.
    发明授权
    Method for producing an optically active β-amino acid 有权
    光学活性β-氨基酸的制造方法

    公开(公告)号：US07015348B2

    公开(公告)日：2006-03-21

    申请号：US10628394

    申请日：2003-07-29

    申请人： Kazuhiko Matsumura ,  Xiaoyong Zhang ,  Takao Saito

    发明人： Kazuhiko Matsumura ,  Xiaoyong Zhang ,  Takao Saito

    IPC分类号： C07C229/00

    CPC分类号： C07C227/16 ,  C07B2200/07 ,  C07C227/32 ,  C07C2601/08 ,  C07D333/24 ,  Y02P20/55 ,  C07C229/08 ,  C07C229/34 ,  C07C229/48 ,  C07C229/22

    摘要： To provide a producing method of an optically active β-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on.A producing method of an optically active β-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.

    摘要翻译： 为了提供可用作药物，农药和生理活性物质生产中间体的光学活性β-氨基酸的制备方法，通过高性能和高对映体过量的催化和不对称合成方法，而不需要额外的 程序如引入和去除保护基等。 一种光学活性β-氨基酸的制备方法，其包括使烯胺进行不对称氢化。

    Method for producing an optically active beta-amino acid
    2.
    发明申请
    Method for producing an optically active beta-amino acid 有权
    光学活性β-氨基酸的制造方法

    公开(公告)号：US20060122418A1

    公开(公告)日：2006-06-08

    申请号：US11290440

    申请日：2005-12-01

    申请人： Kazuhiko Matsumura ,  Xiaoyong Zhang ,  Takao Saito

    发明人： Kazuhiko Matsumura ,  Xiaoyong Zhang ,  Takao Saito

    IPC分类号： C07C227/16

    CPC分类号： C07C227/16 ,  C07B2200/07 ,  C07C227/32 ,  C07C2601/08 ,  C07D333/24 ,  Y02P20/55 ,  C07C229/08 ,  C07C229/34 ,  C07C229/48 ,  C07C229/22

    摘要： The Problem to Be Solved: To provide a producing method of an optically active β-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on. Means to Solve the Problems: A producing method of an optically active β-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.

    摘要翻译： 要解决的问题：通过高性能和高性能的催化和不对称合成方法提供可用作药物，农药和生理活性物质生产中间体的光学活性β-氨基酸的制备方法 对映异构体过量，而不需要额外的方法，例如引入和除去保护基等。 解决问题的手段：光学活性β-氨基酸的制备方法，其包括使烯胺进行不对称氢化。

    Phosphine compound, complex containing the phosphine compound as ligand, process for producing optically active aldehyde using the phosphine compound or the complex, and 4-[(R)-1'-formylethyl]azetidin-2-one derivatives
    5.
    发明授权
    Phosphine compound, complex containing the phosphine compound as ligand, process for producing optically active aldehyde using the phosphine compound or the complex, and 4-[(R)-1'-formylethyl]azetidin-2-one derivatives 失效
    膦化合物，含膦化合物作为配体的络合物，使用膦化合物或络合物制备旋光醛的方法，以及4 - [（R）-1'-甲酰基乙基]氮杂环丁-2-酮衍生物

    公开(公告)号：US5530150A

    公开(公告)日：1996-06-25

    申请号：US323492

    申请日：1994-10-12

    申请人： Hidemasa Takaya ,  Nozomu Sakai ,  Kyoko Tamao ,  Satoshi Mano ,  Hidenori Kumobayashi ,  Tetsuo Tomita ,  Takao Saito ,  Kazuhiko Matsumura ,  Yasushi Kato ,  Noboru Sayo

    发明人： Hidemasa Takaya ,  Nozomu Sakai ,  Kyoko Tamao ,  Satoshi Mano ,  Hidenori Kumobayashi ,  Tetsuo Tomita ,  Takao Saito ,  Kazuhiko Matsumura ,  Yasushi Kato ,  Noboru Sayo

    IPC分类号： C07F9/02 ,  C07F15/00

    CPC分类号： C07F9/02 ,  C07F15/00

    摘要： A phosphine compound represented by one of the formulas: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represent a phenyl group or a phenyl group substituted with a halogen atom or a lower alkyl group or taken together form a divalent hydrocarbon group; and R.sup.3 and R.sup.4, which may be the same or different, each represent a lower alkyl group, a phenyl group or a phenyl group substituted with a halogen atom, a lower alkyl group or a lower alkoxy group or taken together form a divalent hydrocarbon group, and wherein R.sup.6 and R.sup.6' which may be the same or different, each represent a hydrogen atom, a lower alkyl group or a lower alkoxy group; R.sup.5, R.sup.5', R.sup.11 and R.sup.11' which may be the same or different, each represent a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; or a pair of R.sup.5 and R.sup.6 or a pair of R.sup.5' and R.sup.6' may form a ring; R.sup.7 and R.sup.8, which may be the same or different, each represent a phenyl group or a phenyl group substituted with a lower alkyl group, a halogen atom or a lower alkoxy group; and R.sup.9 and R.sup.10, which may be the same or different, each represent a phenyl group or a phenyl group substituted with a lower alkyl group, a lower alkoxy group or a halogen atom; or R.sup.9 and R.sup.10 may be taken together to form a divalent hydrocarbon group.

    摘要翻译： 由下式之一表示的膦化合物：其中R 1和R 2可以相同或不同，各自表示苯基或苯基（III），其中R 1和R 2可以相同或不同， 被卤素原子或低级烷基取代或一起形成二价烃基; 和可以相同或不同的R 3和R 4各自表示低级烷基，苯基或被卤素原子，低级烷基或低级烷氧基取代的苯基或一起形成二价烃基 并且其中可以相同或不同的R6和R6'各自表示氢原子，低级烷基或低级烷氧基; R5，R5'，R11和R11'可以相同或不同，分别表示氢原子，低级烷基，低级烷氧基或卤素原子; 或一对R 5和R 6或一对R 5'和R 6'可以形成环; R 7和R 8可以相同或不同，表示苯基或被低级烷基，卤原子或低级烷氧基取代的苯基; 和R 9和R 10可以相同或不同，各自表示苯基或被低级烷基，低级烷氧基或卤素原子取代的苯基; 或者R 9和R 10可以一起形成二价烃基。

    Asymmetric reductive amination of keto acid derivatives for producing amino acid derivatives
    6.
    发明授权
    Asymmetric reductive amination of keto acid derivatives for producing amino acid derivatives 有权
    用于生产氨基酸衍生物的酮酸衍生物的不对称还原胺化

    公开(公告)号：US07626034B2

    公开(公告)日：2009-12-01

    申请号：US10571855

    申请日：2004-09-17

    申请人： Kazuhiko Matsumura ,  Takao Saito

    发明人： Kazuhiko Matsumura ,  Takao Saito

    IPC分类号： C07D211/70

    CPC分类号： C07D333/36 ,  C07B2200/07 ,  C07C227/08 ,  C07C227/32 ,  C07C229/08 ,  C07C229/22 ,  C07C229/34

    摘要： The present invention relates to a process for producing amino acid derivatives such as optically active β-amino acid in short steps with good yield and high optical purity, which comprises reacting a keto acid of the formula (1): wherein R1 is hydrogen, an optionally substituted hydrocarbon, etc.; R2 is a spacer; and R3 is an optionally substituted alkoxy, etc., or a salt thereof, with ammonia or an amine or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid and/or a fluorine-containing alcohol, to give an amino acid derivative of the formula (2): wherein Q is a group formed by removing one hydrogen atom from ammonia or an amine; X′ is an acid and/or a fluorine-containing alcohol; and b is 0 or 1.

    摘要翻译： 本发明涉及一种具有良好产率和高光学纯度的短程度生产氨基酸衍生物如光学活性β-氨基酸的方法，其包括使式（1）的酮酸反应：其中R1是氢， 任选取代的烃类等; R2是间隔物; 和R3是任选取代的烷氧基等，或其盐与氨或胺或其盐在手性催化剂的存在下和在存在或不存在酸和/或含氟醇的情况下， 得到式（2）的氨基酸衍生物：其中Q是通过从氨或胺除去一个氢原子而形成的基团; X'是酸和/或含氟醇; b为0或1。

    Process for producing optically active alcohol
    8.
    发明授权
    Process for producing optically active alcohol 有权
    光学活性醇的制造方法

    公开(公告)号：US06492545B2

    公开(公告)日：2002-12-10

    申请号：US09909803

    申请日：2001-07-23

    申请人： Takao Saito ,  Tohru Yokozawa ,  Kazuhiko Matsumura ,  Noboru Sayo

    发明人： Takao Saito ,  Tohru Yokozawa ,  Kazuhiko Matsumura ,  Noboru Sayo

    IPC分类号： C07C6966

    CPC分类号： C07C67/31 ,  C07B2200/07 ,  Y02P20/55 ,  C07C69/675

    摘要： A novel process in which an optically active alcohol compound having a desired absolute configuration and a high optical purity can be obtained by asymmetrically hydrogenating a &bgr;-keto acid compound through a simple operation. An optically active alcohol represented by general formula (III) as defined is obtained by asymmetrically hydrogenating a &bgr;-keto ester compound represented by general formula (I) as defined in the presence of at least one ruthenium complex having as a ligand an optically active tertiary diphosphine compound represented by general formula (II) as defined.

    摘要翻译： 通过简单的操作通过不对称氢化β-酮酸化合物，可以获得具有所需绝对构型和高光学纯度的光学活性醇化合物的新方法。 由通式（III）表示的光学活性醇通过不对称氢化由通式（I）表示的β-酮酯化合物获得，如在至少一种具有光学活性第三级 如通式（Ⅱ）所示的二膦化合物。

    Asymmetric reductive amination of keto acid derivatives for producing amino acid derivatives
    9.
    发明申请
    Asymmetric reductive amination of keto acid derivatives for producing amino acid derivatives 有权
    用于生产氨基酸衍生物的酮酸衍生物的不对称还原胺化

    公开(公告)号：US20070142443A1

    公开(公告)日：2007-06-21

    申请号：US10571855

    申请日：2004-09-17

    申请人： Kazuhiko Matsumura ,  Takao Saito

    发明人： Kazuhiko Matsumura ,  Takao Saito

    IPC分类号： A61K31/44 ,  A61K31/40 ,  A61K31/24 ,  C07D213/55 ,  C07C229/02

    CPC分类号： C07D333/36 ,  C07B2200/07 ,  C07C227/08 ,  C07C227/32 ,  C07C229/08 ,  C07C229/22 ,  C07C229/34

    摘要： The present invention relates to a process for producing amino acid derivatives such as optically active β-amino acid in short steps with good yield and high optical purity, which comprises reacting a keto acid of the formula (1): wherein R1 is hydrogen, an optionally substituted hydrocarbon, etc.; R2 is a spacer; and R3 is an optionally substituted alkoxy, etc., or a salt thereof, with ammonia or an amine or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid and/or a fluorine-containing alcohol, to give an amino acid derivative of the formula (2): wherein Q is a group formed by removing one hydrogen atom from ammonia or an amine; X′ is an acid and/or a fluorine-containing alcohol; and b is 0 or 1.

    摘要翻译： 本发明涉及以简单的步骤生产氨基酸衍生物如光学活性β-氨基酸的方法，该方法具有良好的产率和高的光学纯度，其包括使式（1）的酮酸：其中R 1 氢，任选取代的烃等; R 2是间隔物; R 3是任选取代的烷氧基等，或其盐与氨或胺或其盐在手性催化剂的存在下和存在或不存在酸和 /或含氟醇，得到式（2）的氨基酸衍生物：其中Q是通过从氨或胺除去一个氢原子而形成的基团; X'是酸和/或含氟醇; b为0或1。