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1. 发明授权

EP1088820B1 PROCESS FOR THE PREPARATION OF 3-HYDROXYTETRAHYDROFURAN 有权
标题翻译：用于生产3-羟基
公开(公告)号：EP1088820B1
公开(公告)日：2004-02-18
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.

2. 发明公开

EP1179530A1 PROCESSES FOR PREPARING OPTICALLY ACTIVE AMINO ACID DERIVATIVES 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG OPTISCH AKTIVERAMINOSÄUREDERIVATE
公开(公告)号：EP1179530A1
公开(公告)日：2002-02-13
申请号：EP01904517.8
申请日：2001-02-16
申请人： Kaneka Corporation
发明人： SUGAWARA, Masanobu , FUJII, Akio , OKURO, Kazumi , SAKA, Yasuhiro , NAGASHIMA, Nobuo , INOUE, Kenji , TAKEDA, Toshihiro , KINOSHITA, Koichi , MOROSHIMA, Tadashi , FUSE, Yoshihide , UEDA, Yasuyoshi
IPC分类号： C07D203/08 , C07D203/24 , C07C227/04 , C07C227/10 , C07C229/26 , C07C311/19 , C07B53/00
CPC分类号： C07D203/08 , C07B2200/07 , C07C227/10 , C07C227/32 , C07C227/42 , C07C229/30 , C07C303/36 , C07D203/20 , C07D203/24 , C07C311/19 , C07C229/26
摘要： An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent.
According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要翻译：光学活性氨基酸衍生物是通过N-保护光学活性3-卤代丙氨酸衍生物进行环化，或环化该衍生物进行N-保护而得到光学活性N-保护的氮丙啶-2-羧酸衍生物在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物，或通过N-保护光学活性3-卤代丙氨酸衍生物，由此得到N-保护的氮丙啶 -2-羧酸，其在2-和/或4-位被硝基取代的苯磺酰基保护，然后用有机金属试剂处理该产物。根据该方法，可以通过简单的方法从便宜的材料制备天然和非天然旋光氨基酸。

3. 发明公开

EP0930292A1 PROCESS FOR PREPARING $g(b)-AMINO-$g(a)-HYDROXY ACID DERIVATIVES 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON BETA-AMINO-ALPHA-HYDROXYCARBONSAEURE-DERIVATEN
公开(公告)号：EP0930292A1
公开(公告)日：1999-07-21
申请号：EP97935797.7
申请日：1997-08-18
申请人： KANEKA CORPORATION
发明人： MATSUMOTO, Shingo , MATSUO, Kazuhiko , SUGAWA, Tadashi , MOROSHIMA, Tadashi , INOUE, Kenji
IPC分类号： C07C229/22 , C07C229/34 , C07C227/02 , C07D209/48
CPC分类号： C07C303/44 , C07C227/02 , C07C227/42 , C07C269/08 , C07C271/18 , C07C303/40 , C07D209/26 , Y02P20/55 , C07C311/19 , C07C229/22 , C07C229/34
摘要： An object of the present invention is to provide a process for producing a β-amino-α-hydroxy acid derivative via efficient and industrially utilizable steps.
The present invention provides a process for producing a β-amino-α-hydroxy acid derivative represented by the general formula (2) given below which comprises hydrolyzing an α-amino-α',α'-dihaloketone derivative of the general formula (1) given below in the presence of a base, followed by protecting the amino group or without protecting the same.
摘要翻译：本发明的目的是提供一种通过有效和可工业利用的步骤生产β-氨基-α-羟基酸衍生物的方法。本发明提供一种制备由下述通式（2）表示的β-氨基-α-羟基酸衍生物的方法，其包括水解通式（1）的α-氨基-α'，α'-二卤代酮衍生物），然后保护氨基或不保护氨基。

4. 发明公开

EP0827943A1 PROCESSES FOR THE REDUCTION OF CARBONYL COMPOUNDS 失效
标题翻译： VERFAHREN ZUR REDUKTION VON CARBONYLVERBINDUNGEN
公开(公告)号：EP0827943A1
公开(公告)日：1998-03-11
申请号：EP97901761.3
申请日：1997-01-29
申请人： KANEKA CORPORATION
发明人： SUGAWA, Tadashi , MOROSHIMA, Tadashi , INOUE, Kenji , KAN, Kazunori
IPC分类号： C07B41/02 , C07C29/143 , C07C33/22 , C07C213/00 , C07C215/28 , C07C271/10 , C07C323/43
CPC分类号： C07B53/00 , C07B41/02 , C07C29/143 , C07C213/00 , C07C269/06 , C07C319/20 , C07C323/43 , C07C271/16 , C07C271/22 , C07C33/22 , C07C33/46
摘要： The present invention provides a process for reducing carbonyl compounds to hydroxy compounds, in particular stereoselectively reducing α-aminohaloketone derivatives, under mild conditions in an easy and simple manner, which comprises reacting a carbonyl compound of the general formula (1) with an organoaluminum compound of the general formual (4) to provide the corresponding alcohol compound of the general formula (5).
摘要翻译：本发明提供了一种在温和条件下以容易和简单的方式将羰基化合物还原成羟基化合物，特别是立体选择性还原α-氨基卤代酮衍生物的方法，其包括使通式（1）的羰基化合物与有机铝化合物的通式（4）提供相应的通式（5）的醇化合物。

5. 发明授权

EP1035131B1 PROCESS FOR THE PREPARATION OF N2 -(1(S)-CARBOXY-3-PHENYLPROPYL)-L-LYSYL-L-PROLINE 有权
标题翻译：用于生产N2-（1（S）羧基-3-苯丙基）-L-赖氨酰-L-脯氨酸
公开(公告)号：EP1035131B1
公开(公告)日：2006-11-22
申请号：EP99944783.2
申请日：1999-09-22
申请人： KANEKA CORPORATION
发明人： MOROSHIMA, Tadashi , YANAGIDA, Yoshifumi , FUSE, Yoshihide , UEDA, Yasuyoshi
IPC分类号： C07K5/068 , C07K5/06
CPC分类号： C07K5/0222
摘要： 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.

6. 发明授权

EP0967221B1 PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS 失效
标题翻译： METHOD FOR PRODUCING药理学上可接受的N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰基氨基酸盐
公开(公告)号：EP0967221B1
公开(公告)日：2005-05-25
申请号：EP98932585.7
申请日：1998-07-21
申请人： KANEKA CORPORATION
发明人： UEDA, Yasuyoshi , KINOSHITA, Koichi , MOROSHIMA, Tadashi , YANAGIDA, Yoshifumi , FUSE, Yoshihide
IPC分类号： C07K5/062 , C07K1/02 , C07K1/08
CPC分类号： C07K5/0222 , C07K5/06026
摘要： 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.

7. 发明公开

EP1386918A1 METHOD FOR OBTAINING OPTICALLY ACTIVE EPOXIDE 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG OPTISCH AKTIVER EPOXIDE
公开(公告)号：EP1386918A1
公开(公告)日：2004-02-04
申请号：EP02724758.4
申请日：2002-05-10
申请人： KANEKA CORPORATION
发明人： MOROSHIMA, Tadashi , UEDA, Yasuyoshi
IPC分类号： C07D301/32 , C07D303/08
CPC分类号： C07D301/36 , C07D301/32 , C07D303/08
摘要： 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.
摘要翻译：本发明提供了一种能够抑制在光学活性环氧化物蒸馏期间由于暴露于热量而导致光学纯度降低的方法，以便以工业规模简单地获得高质量的光学活性环氧化物。在该方法中，在碱的存在下蒸发光学活性环氧化物以抑制光学纯度的降低。

8. 发明授权

EP0827943B1 PROCESSES FOR THE REDUCTION OF CARBONYL COMPOUNDS 失效
标题翻译：一种用于减少羰基
公开(公告)号：EP0827943B1
公开(公告)日：2003-05-21
申请号：EP97901761.3
申请日：1997-01-29
申请人： KANEKA CORPORATION
发明人： SUGAWA, Tadashi , MOROSHIMA, Tadashi , INOUE, Kenji , KAN, Kazunori
IPC分类号： C07B41/02 , C07C29/143 , C07C33/22 , C07C213/00 , C07C215/28 , C07C271/10 , C07C323/43
CPC分类号： C07B53/00 , C07B41/02 , C07C29/143 , C07C213/00 , C07C269/06 , C07C319/20 , C07C323/43 , C07C271/16 , C07C271/22 , C07C33/22 , C07C33/46

9. 发明公开

EP0967221A1 PROCESS FOR PREPARING PHARMACOLOGICALLY ACCEPTABLE SALTS OF N-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-L-ALANYL AMINO ACIDS 失效
标题翻译： METHOD FOR PRODUCING药理学上可接受的N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰基氨基酸盐
公开(公告)号：EP0967221A1
公开(公告)日：1999-12-29
申请号：EP98932585.7
申请日：1998-07-21
申请人： KANEKA CORPORATION
发明人： UEDA, Yasuyoshi , KINOSHITA, Koichi , MOROSHIMA, Tadashi , YANAGIDA, Yoshifumi , FUSE, Yoshihide
IPC分类号： C07K5/062 , C07K1/02 , C07K1/08
CPC分类号： C07K5/0222 , C07K5/06026
摘要： 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.
摘要翻译：在与N-氨基酸（1（S）乙氧基羰基-3-冷凝：一种用于制备药学上可接受的N-（1（S）乙氧基羰基-3-苯丙基）-L-丙氨酰氨基酸，其包括以下步骤的过程的盐在碱性条件下苯丙基）-L-丙氨酸的N-羧基酸酐; 在中性脱羧缩合物在酸性条件以制备N-（1（S） - 乙氧羰基-3-苯丙基）-L-丙氨酰基氨基酸; 和将产物转化为药学上可接受的盐，其特征在于在做了一系列的程序到一药理学上可接受的盐的形成或高达药学上可接受的盐是在wässrige液体中进行的撤出，以抑制生产的副产物（3）。。根据该方法中，N-高质量药理学上可接受的盐（1（S）乙氧基羰基-3-苯丙基）-L-丙氨酰基氨基酸可以以高产率以具有成本效益的方式在商业规模上制备。

10. 发明授权

EP2842950B1 METHOD FOR PRODUCING COMPOSITION CONTAINING FUCOXANTHIN 有权
公开(公告)号：EP2842950B1
公开(公告)日：2018-09-19
申请号：EP13782097.3
申请日：2013-02-27
申请人： Kaneka Corporation
发明人： UEKITA, Ken , MOROSHIMA, Tadashi
IPC分类号： C07D301/32 , C07D303/32 , A61K8/49 , A61K31/336 , A61P3/04 , A61P3/10 , A61P29/00 , A61P35/00
CPC分类号： C07D301/32 , A23L33/10 , A61K8/4973 , A61K31/336 , A61K2800/10 , A61Q19/00 , C07D303/32
摘要： A method for producing a composition containing fucoxanthin includes a first step of adding a water-soluble solvent containing 0 to 80% by weight of water to seaweed to obtain a seaweed component extract, and then adding water and/or a water-soluble solvent to the seaweed component extract in such a manner that the concentration of the water-soluble solvent is 20 to 45% by weight and also adding a diluent thereto to obtain a diluent-containing extract, and a second step of stirring the diluent-containing extract, and then collecting a substance aggregating into the diluent-containing extract as a composition containing fucoxanthin by separation.

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