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    Process for producing N-(D-.alpha.-methyl-.beta.-mercaptopropionyl)-L-proline and its intermediate
    1.
    发明授权
    Process for producing N-(D-.alpha.-methyl-.beta.-mercaptopropionyl)-L-proline and its intermediate 失效
    制备N-（D-α-甲基-β-巯基丙酰基）-L-脯氨酸及其中间体的方法

    公开(公告)号：US5917055A

    公开(公告)日：1999-06-29

    申请号：US849337

    申请日：1997-07-31

    申请人： Yasuyoshi Ueda ,  Fumihiko Kanou ,  Koichi Kinoshita ,  Takahiro Okubo

    发明人： Yasuyoshi Ueda ,  Fumihiko Kanou ,  Koichi Kinoshita ,  Takahiro Okubo

    IPC分类号： A61K31/00 ,  C07D207/16

    CPC分类号： C07D207/16

    摘要： A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide and an L-proline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with active carbon or crystallization followed by deacylation. In the formula, R.sup.1 represents acyl and n represents an integer of from 2 to 4. ##STR1##

    摘要翻译： PCT No.PCT / JP96 / 02902 Sec。 371日期1997年7月31日 102（e）1997年7月31日PCT PCT 1996年10月7日PCT公布。 公开号WO97 / 12858 日期1997年04月10日在高产量的高品质卡托普利经济地生产方法中高度方便和高效的方法，其显着降低了杂质含量，并且具有高熔点和用于合成它们的中间体，其仅含有少量的 前体作为杂质，具有优良的品质。 该方法包括使酰卤和L-脯氨酸进行Schotten-Baumann反应，并通过在通式（5）或（6）表示的前体中处理， 在Schotten-Baumann反应之后，将含有活性炭的水介质溶液或结晶，然后脱酰基化。 式中，R1表示酰基，n表示2〜4的整数。

    Simple process for producing high quality captopril
    2.
    发明授权
    Simple process for producing high quality captopril 失效
    生产高品质卡托普利的简单过程

    公开(公告)号：US06187932B1

    公开(公告)日：2001-02-13

    申请号：US09077747

    申请日：1998-08-03

    申请人： Koichi Kinoshita ,  Fumihiko Kano ,  Takahiro Okubo ,  Yasuyoshi Ueda

    发明人： Koichi Kinoshita ,  Fumihiko Kano ,  Takahiro Okubo ,  Yasuyoshi Ueda

    IPC分类号： C07D20712

    CPC分类号： C07D207/16

    摘要： A process for producing captopril of the following formula (1) comprising subjecting a substrate compound of the following general formula (2) to a hydrolysis reaction in aqueous medium to remove the RCO group and isolating the product compound, said hydrolysis reaction in aqueous medium being conducted in the presence of a strong acid at pH not over 1 and a reaction temperature not below 40° C.

    摘要翻译： 一种制备下式（1）的卡托普利的方法，包括使下列通式（2）的底物化合物在水性介质中进行水解反应以除去RCO基团并分离产物化合物，水介质中的所述水解反应为 在pH不超过1，反应温度不低于40℃的强酸存在下进行。

    Method for isolation of n-protected s-phenylcysteine
    5.
    发明授权
    Method for isolation of n-protected s-phenylcysteine 失效
    用于分离正保护的S-苯基半胱氨酸的方法

    公开(公告)号：US06320072B1

    公开(公告)日：2001-11-20

    申请号：US09646702

    申请日：2000-12-14

    申请人： Yasuyoshi Ueda ,  Hiroshi Murao ,  Koki Yamashita ,  Koichi Kinoshita

    发明人： Yasuyoshi Ueda ,  Hiroshi Murao ,  Koki Yamashita ,  Koichi Kinoshita

    IPC分类号： C07C32100

    CPC分类号： C07C319/28 ,  Y02P20/55 ,  C07C323/59

    摘要： This invention provides a method of isolating N-protected-S-phenylcysteine (1) of high purity, expediently, efficiently and in good yield, which comprises causing said N-protected-S-phenylcysteine to be salted out in the form of a base salt in the presence of water. wherein R1 represents an amino-protecting group; R2 represents a hydrogen atom or, either independently of R1 or taken together with R1, represents an amino-protecting group.

    摘要翻译： 本发明提供了一种方法，有效和高效分离高纯度N-保护的S-苯基半胱氨酸（1）的方法，其包括使所述N-保护的S-苯基半胱氨酸以碱的形式盐析 盐，其中R 1表示氨基保护基; R 2表示氢原子，或独立地为R 1或与R 1一起表示氨基保护基。

    Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid
    7.
    发明授权
    Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效
    制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐的方法

    公开(公告)号：US06713628B2

    公开(公告)日：2004-03-30

    申请号：US10295897

    申请日：2002-11-18

    申请人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    发明人： Yasuyoshi Ueda ,  Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Yoshihide Fuse

    IPC分类号： C07D20704

    CPC分类号： C07K5/0222 ,  C07K5/06026

    摘要： There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

    摘要翻译： 提供了制备N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法，其包括将氨基酸和N-（1（S） - 乙氧基羰基 - 3-苯基丙基）-L-丙氨酸N-羧酸酐，在中性和酸性条件下进行脱羧，得到N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸，和 形成其药理学上可接受的盐，其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物（3）的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-（1（S） - 乙氧基羰基-3-苯基丙基）-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

    Processes for producing &bgr;-halogeno-&agr;-amino-carboxylic acids and phenylcysteine derivatives and intermediates thereof
    8.
    发明授权
    Processes for producing &bgr;-halogeno-&agr;-amino-carboxylic acids and phenylcysteine derivatives and intermediates thereof 失效
    制备β-卤代-α-氨基 - 羧酸和苯基半胱氨酸衍生物的方法及其中间体

    公开(公告)号：US06372941B1

    公开(公告)日：2002-04-16

    申请号：US09582461

    申请日：1999-08-16

    申请人： Koki Yamashita ,  Kenji Inoue ,  Koichi Kinoshita ,  Yasuyoshi Ueda ,  Hiroshi Murao

    发明人： Koki Yamashita ,  Kenji Inoue ,  Koichi Kinoshita ,  Yasuyoshi Ueda ,  Hiroshi Murao

    IPC分类号： C07C22900

    CPC分类号： C07C227/16 ,  C07C319/14 ,  Y02P20/55 ,  C07C323/58 ,  C07C323/59 ,  C07C229/20

    摘要： An industrially advantageous method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized. A method of producing &bgr;-halogeno-&agr;-aminocarboxylic acids or salts thereof is disclosed which comprises halogenating the hydroxyl group of a &bgr;-hydroxy-&agr;-aminocarboxylic acid (in which the basicity of the amino group in &agr;-position is not masked by the presence of a substituent on said amino group) or a salt thereof with an acid with a halogenating agent. A method of producing optically active N-protected-S-phenylcysteines represented by the general formula (3) or salts thereof is further disclosed which comprises applying the above production method to optically active serine or a salt thereof and then carrying out treatment with an amino-protecting agent and reaction with thiophenol under a basic condition.

    摘要翻译： 提供了产生β-卤代-α-氨基羧酸的工业上有利的方法。 还提供了分别制备具有高光学纯度的光学活性N-保护的S-苯基半胱氨酸及其中间体的方法，其中使用上述制备方法.1。制备β-卤代-α-氨基羧酸或其盐的方法 其中包括将β-羟基-α-氨基羧酸的羟基（其中在所述氨基上不存在取代基的α-位置上的氨基的碱性）或其盐与卤素化反应 具有卤化剂的酸。 进一步公开了制备由通式（3）表示的光学活性N-保护的S-苯基半胱氨酸或其盐的方法，其包括将上述制备方法应用于光学活性丝氨酸或其盐，然后用氨基 保护剂和与苯硫酚在基本条件下的反应。

    Process for the preparation of 3-hydroxytetrahydrofuran
    9.
    发明授权
    Process for the preparation of 3-hydroxytetrahydrofuran 失效
    3-羟基四氢呋喃的制备方法

    公开(公告)号：US06359155B1

    公开(公告)日：2002-03-19

    申请号：US09719686

    申请日：2001-02-15

    申请人： Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Nobuo Nagashima ,  Yasuhiro Saka ,  Tatsuya Honda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    发明人： Koichi Kinoshita ,  Tadashi Moroshima ,  Yoshifumi Yanagida ,  Nobuo Nagashima ,  Yasuhiro Saka ,  Tatsuya Honda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    IPC分类号： C07D30720

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

    摘要： An industrial advantage process for producing high-purity 3-hydroxytetrahydrofuran easily and simply, which comprises reducing a 4-halo-3-hydroxybutyric acid ester (1) with a boron hydride compound and/or an aluminum hydride compound as a reducing agent in an organic solvent immiscible with water; treating the reaction mixture with an acid and water to thereby effect conversion to the corresponding 4-halo-1,3-butanediol and at the same time giving an aqueous solution containing said compound; carrying out the cyclization reaction of the 4-halo-1,3-butanediol in said aqueous solution; extracting the resulting 3-hydroxytetrahydrofuran from the 3-hydroxytetrahydrofuran-containing aqueous solution using an organic solvent immiscible with water; and isolating the 3-hydroxytetrahydrofuran by concentration and/or distillation of the solution obtained.

    摘要翻译： 用于容易且简单地生产高纯度3-羟基四氢呋喃的工业优势方法，其包括用硼氢化合物和/或氢化铝化合物作为还原剂还原4-卤代-3-羟基丁酸酯（1） 与水不混溶的有机溶剂;用酸和水处理反应混合物，从而转化为相应的4-卤代-1,3-丁二醇，同时得到含有所述化合物的水溶液;进行环化反应 所述水溶液中的4-卤代-1,3-丁二醇;使用与水不混溶的有机溶剂从含3-羟基四氢呋喃的水溶液中萃取所得3-羟基四氢呋喃; 通过所得溶液的浓缩和/或蒸馏来使3-羟基四氢呋喃分离。