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    32.
    发明专利
    未知

    公开(公告)号：DE60207233D1

    公开(公告)日：2005-12-15

    申请号：DE60207233

    申请日：2002-05-10

    Applicant: KANEKA CORP

    Inventor： MOROSHIMA TADASHI ,  UEDA YASUYOSHI

    IPC: C07D301/03 ,  C07D301/32 ,  C07D301/36 ,  C07D303/08

    Abstract: The present invention provides a method capable of suppressing a decrease in optical purity due to the exposure to heat during distillation of an optically active epoxide to permit an optically active epoxide of high quality to be simply obtained on an industrial scale. In the method, an optically active epoxide is distilled in the presence of a base to suppress a decrease in optical purity.

    33.
    发明专利
    未知

    公开(公告)号：DE69830307D1

    公开(公告)日：2005-06-30

    申请号：DE69830307

    申请日：1998-07-21

    Applicant: KANEKA CORP

    Inventor： UEDA YASUYOSHI ,  KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  YANAGIDA YOSHIFUMI ,  FUSE YOSHIHIDE

    IPC: A61P9/12 ,  C07K1/02 ,  C07K1/08 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062

    Abstract: Preparation of salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acid derivatives of formula (R1)NH-CH(R2)-CO2H (I) comprises: (a) condensing an amino acid with N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxyanhydride of formula (II), under basic conditions; (b) decarboxylating the condensate under neutral to acidic conditions to give (I); and (c) and converting (I) to its salt. Steps (a), (b) and optionally (c) are carried out in aqueous liquid to inhibit the formation of by-products of formula (III): -N(R1)CH(R2)-C(O)- = e.g. group of formula (i).

    Process for preparing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline
    37.
    发明专利
    Process for preparing N2-(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline 未知

    公开(公告)号：CZ20001897A3

    公开(公告)日：2000-10-11

    申请号：CZ20001897

    申请日：1999-09-22

    Applicant: KANEKA CORP

    Inventor： MOROSHIMA TADASHI ,  YANAGIDA YOSHIFUMI ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

    IPC: C07K5/068 ,  A61K38/05 ,  A61P9/12 ,  C07K5/02

    Abstract: The process for producing N -(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline in a simple, efficient and industrially advantageous manner, which comprises: the first step of subjecting the N -(1(S)-alkoxycarbonyl-3-phenylpropyl)-N -trifluoroacetyl-L-lysyl -L-proline (1) to alkali hydrolysis in a mixed solution composed of water and a hydrophilic organic solvent using an inorganic base in an amount of n molar equivalents (n >/= 3) per mole of the above compound (1), the second step of neutralizing the hydrolysis product using an inorganic acid in an amount of (n - 1) to n molar equivalents (n >/= 3) and removing the inorganic salt formed by causing the same to precipitate out from a solvent system suited for decreasing the solubility of the inorganic salt, and the third step of causing the compound (2) existing in the mixture after removal of the inorganic salt to crystallize out at the isoelectric point thereof and thereby recovering the compound (2) in the form of crystals while retaining the salts comprising the trifluoroacetic acid-derived organic acid salt in a state dissolved in the mother liquor.

    PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS
    39.
    发明专利
    PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS 未知

    公开(公告)号：CA2266757A1

    公开(公告)日：1999-02-04

    申请号：CA2266757

    申请日：1998-07-21

    Applicant: KANEKA CORP

    Inventor： UEDA YASUYOSHI ,  KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  FUSE YOSHIHIDE ,  YANAGIDA YOSHIFUMI

    IPC: A61P9/12 ,  C07K1/02 ,  C07K1/08 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062

    Abstract: A process for preparing pharmacologically acceptable salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids, comprising the steps of: condensing an amino acid with N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxyanhydride under basic conditions; decarboxylating the condensate under neutral to acidic conditions to prepare an N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acid; and converting the product to a pharmacologically acceptable salt thereof, characterized in that a series of procedures up to the formation of a pharmacologically acceptable salt or up to the withdrawal of the pharmaceutically acceptable salt thereof are carried out in an aqueous liquid to inhibit the production of a by-product (3). According to this process, high-quality pharmacologically acceptable salts of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids can be prepared in high yields in a cost-effective manner on a commercial scale.

    Method for producing optically active n-substituted aminoacyl cyclic urea derivative
    40.
    发明专利
    Method for producing optically active n-substituted aminoacyl cyclic urea derivative 有权
    生产光学活性N-取代氨基酸循环尿素衍生物的方法

    公开(公告)号：JP2007063231A

    公开(公告)日：2007-03-15

    申请号：JP2005254614

    申请日：2005-09-02

    Applicant: Kaneka Corp ,  株式会社カネカ

    Inventor： OISHI TAKAHIRO ,  HIRAI YOSHINORI ,  KAWASAKI HIROAKI ,  MOROSHIMA TADASHI ,  NAGASHIMA NOBUO

    IPC: C07D233/38

    Abstract: PROBLEM TO BE SOLVED: To provide an industrially advantageous method for easily producing an optically active N-substituted aminoacyl cyclic urea derivative or its salt which is a useful medicinal compound known to have strong angiotensin-converting enzyme inhibiting action. SOLUTION: The optically active N-substituted aminoacyl cyclic urea derivative and its salt can be produced without necessitating ultra-low temperature by reacting an optically active cyclic urea carboxylic acid derivative with carboxyl group of an optically active N-substituted amino acid N-carboxylic anhydride or an optically active N-substituted amino acid derivative. COPYRIGHT: (C)2007,JPO&INPIT

    Abstract translation: 要解决的问题：提供一种工业上有利的方法，用于容易地制备已知具有强的血管紧张素转化酶抑制作用的有用的药物化合物的光学活性N-取代的氨基酰基环脲衍生物或其盐。 解决方案：光学活性的N-取代的氨基酰基环脲衍生物及其盐可以通过光学活性的环状脲羧酸衍生物与光学活性的N-取代的氨基酸N的羧基反应而不需要超低温来制备 羧酸酐或光学活性N-取代氨基酸衍生物。 版权所有（C）2007，JPO＆INPIT

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