公开(公告)号：EP1386918A4

公开(公告)日：2004-05-26

申请号：EP02724758

申请日：2002-05-10

Applicant: KANEKA CORP

Inventor： MOROSHIMA TADASHI ,  UEDA YASUYOSHI

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

CPC classification number: C07D301/36 ,  C07D301/32 ,  C07D303/08

Abstract: A method for obtaining an epoxide having high optical purity, characterized in that an optically active epoxide is subjected to a distillation in the presence of a base. The method allows the suppression of the decrease of optical purity due to the exposure to heat during the distillation of an optically active epoxide, and thus can be employed for producing an optically active epoxide of high quality with ease and simplicity on an industrial scale.

Abstract translation: 一种获得具有高光学纯度的环氧化物的方法，其特征在于光学活性环氧化物在碱存在下进行蒸馏。 该方法可以抑制光学活性环氧化物蒸馏过程中由于暴露于热而引起的光学纯度的降低，因此可用于在工业规模上简单且简单地制备高质量的光学活性环氧化物。

公开(公告)号：EP1088820A4

公开(公告)日：2001-08-16

申请号：EP00915524

申请日：2000-04-14

Applicant: KANEKA CORP

Inventor： KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  YANAGIDA YOSHIFUMI ,  NAGASHIMA NOBUO ,  SAKA YASUHIRO ,  HONDA TATSUYA ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

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

CPC classification number: C07C29/147 ,  C07B2200/07 ,  C07D307/20 ,  Y02P20/55 ,  C07C31/42

Abstract: 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.

公开(公告)号：EP2623513A4

公开(公告)日：2014-03-05

申请号：EP11829353

申请日：2011-09-30

Applicant: KANEKA CORP

Inventor： IZUMIDA MASASHI ,  KAWASAKI HIROAKI ,  MOROSHIMA TADASHI

IPC: C07K11/02 ,  C07K1/14

CPC classification number: C07K1/145 ,  C07K1/36 ,  C07K7/06

公开(公告)号：EP2058299A4

公开(公告)日：2009-09-30

申请号：EP07806343

申请日：2007-08-30

Applicant: KANEKA CORP ,  OSAKA SYNTHETIC CHEMICAL LAB I

Inventor： SENO KUNIHIKO ,  OKUDA MASAO ,  KAWASAKI HIROAKI ,  MOROSHIMA TADASHI ,  UEDA YASUYOSHI

IPC: C07C267/00

CPC classification number: C07C267/00

公开(公告)号：EP1018516A4

公开(公告)日：2004-05-26

申请号：EP99929893

申请日：1999-07-19

Applicant: KANEKA CORP

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

IPC: A61P9/00 ,  C07K1/00 ,  C07K5/06 ,  C07K5/062 ,  C07K5/02

CPC classification number: C07K5/06026

Abstract: A method for crystallizing the maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (Enalapril) from an aqueous liquid with ease in good yield, which comprises mixing an aqueous liquid containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, maleic acid and a base and having a pH of 4 or more with an acid in an amount of the acid sufficient to convert the base to a neutral salt, to thereby crystallize N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline in the form of a maleic acid salt.

公开(公告)号：EP1035131A4

公开(公告)日：2002-05-02

申请号：EP99944783

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 ,  C07K5/06

CPC classification number: C07K5/0222

Abstract: A process for preparing N -(1(S)-carboxy-3-phenylpropyl)-L-lysyl-L-proline (2) easily, efficiently and industrially advantageously, which comprises: the first step of conducting the alkaline hydrolysis of an N -(1(S)-alkoxycarbonyl-3-phenylpropyl)-N -trifluoroacetyl-L-lysyl-L-proline (1) by the use of n molar equivalents (wherein n >/= 3) of an inorganic base per mol of the compound (1) either in a mixture of water with a hydrophilic organic solvent or in water; the second step of neutralizing the resulting reaction mixture with (n-1) to n molar equivalents (wherein n >/= 3) of an inorganic acid, replacing the solvent system by a suitable one to thereby precipitate an inorganic salt formed by the above neutralization, and separating and removing the salt; and the third step of crystallizing the compound (2) present in the liquid mixture left after the above removal of the salt at its isoelectric point and recovering the compound (2) as a crystal, while salts mainly comprising organic acid salts resulting from trifluoroacetic acid remain dissolved in the mother liquor.

公开(公告)号：EP0967221A4

公开(公告)日：2002-05-02

申请号：EP98932585

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

CPC classification number: C07K5/0222 ,  C07K5/06026

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.

Abstract translation: 制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸的药理学上可接受的盐的方法，包括以下步骤：使氨基酸与N-（1（S） - 乙氧羰基-3 - 苯基丙基）-L-丙氨酸N-羧酸酐在碱性条件下; 在中性至酸性条件下将缩合物脱羧基以制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸; 并将该产物转化成其药理学上可接受的盐，其特征在于在含水液体中进行一系列形成药理学上可接受的盐或直至其药学上可接受的盐的程序，以抑制 一个副产品（3）。 根据该方法，可以以商业规模以高成本效益的方式高产率地制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰氨基酸的高质量药理学上可接受的盐。