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1. 发明授权

US06372941B1 Processes for producing &bgr;-halogeno-&agr;-amino-carboxylic acids and phenylcysteine derivatives and intermediates thereof 失效
标题翻译：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。

2. 发明授权

US06320072B1 Method for isolation of n-protected s-phenylcysteine 失效
标题翻译：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。

3. 发明授权

US07094926B2 Process for producing optically active carboxylic acid substituted in 2-position 失效
公开(公告)号：US07094926B2
公开(公告)日：2006-08-22
申请号：US10182260
申请日：2001-01-25
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C51/58
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

4. 发明申请

US20060247470A1 Process for producing optically active carboxylic acid substituted in 2-position 审中-公开
标题翻译：用于制备2-位取代的光学活性羧酸的方法
公开(公告)号：US20060247470A1
公开(公告)日：2006-11-02
申请号：US11477626
申请日：2006-06-30
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C53/15 , C07C53/16
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).
摘要翻译：在10〜80℃的温度下，向含有光学活性的2-氨基羧酸（4）和质子酸的水溶液中加入亚硝酸盐，后者的酸的量为1〜3当量前者，其质子浓度为0.5〜2mol / kg进行反应，由此制造光学活性的2-羟基羧酸（1）。使亚硫酰氯和碱性化合物作用于化合物（1）以使其氯化，同时反转2-位的构型。因此，引入光学活性的2-氯羧酰氯（5）。将化合物（5）水解以诱导光学活性的2-氯羧酸（2）。使化合物（2）与硫代乙酸盐反应以引入乙酰硫基，同时反转2-位的构型，从而产生光学活性的2-乙酰基硫代羧酸（3）。

5. 发明申请

US20050245764A1 Process for producing optically active 2-substituted carboxylic acid 审中-公开
标题翻译：光学活性2-取代羧酸的制备方法
公开(公告)号：US20050245764A1
公开(公告)日：2005-11-03
申请号：US10486085
申请日：2002-08-08
申请人： Koki Yamashita , Toshihiro Takeda , Koichi Kinoshita , Yasuyoshi Ueda
发明人： Koki Yamashita , Toshihiro Takeda , Koichi Kinoshita , Yasuyoshi Ueda
IPC分类号： C07C51/363 , C07C51/43 , C07C51/48 , C07C57/58 , C07C67/52 , C07C67/58 , C07C303/28 , C07C303/30 , C07C309/66 , C07C53/15 , C07C53/16
CPC分类号： C07C303/30 , C07B2200/07 , C07C51/363 , C07C51/43 , C07C51/48 , C07C57/58 , C07C67/52 , C07C67/58 , C07C303/28 , Y02P20/55 , C07C69/732 , C07C309/66
摘要： The present invention relates to a process for efficiently producing an optically active 2-bromocarboylic acid and an optically active 2-sulfonyloxycarboxylic acid, which are important in the production of medicinal compounds and so forth. An optically active 2-sulfonyloxycarboxylic acid ester is subjected to deprotection under acid conditions to obtain an optically active 2-sulfonyloxycarboxylic acid. A metal bromide is caused to act on the acid to brominate it with configuration inversion at position 2 to thereby produce an optically active 2-bromocarboxylic acid. The resultant optically active 2-bromocarboxylic acid is isolated/purified by subjecting it to a step in which the acid is crystallized and separated as a salt with a base. Thus, an optically active 2-bromocarboxylic acid having a high chemical purity and high optical purity can be produced.
摘要翻译：本发明涉及一种在制备药物化合物等方面有效生产光学活性的2-溴羧酸和光学活性的2-磺酰氧基羧酸的方法。光学活性的2-磺酰氧基羧酸酯在酸性条件下进行脱保护，得到光学活性的2-磺酰氧基羧酸。使金属溴化物作用于酸，使其在位置2处具有配置倒置溴化，从而产生光学活性的2-溴羧酸。所得光学活性2-溴羧酸通过使其结晶并与碱分离的步骤进行分离/纯化。因此，可以制备具有高化学纯度和高光学纯度的光学活性的2-溴羧酸。

6. 发明授权

US07109352B2 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US07109352B2
公开(公告)日：2006-09-19
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D203/02 , C07D203/08
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。

7. 发明申请

US20050143586A1 Process for producing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US20050143586A1
公开(公告)日：2005-06-30
申请号：US10716430
申请日：2003-11-20
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07C227/10 , C07C227/32 , C07C227/42 , C07C229/26 , C07C229/30 , C07C303/36 , C07C311/19 , C07D203/08 , C07D203/20 , C07D203/24 , C07D203/16
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通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性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。

8. 发明授权

US06720449B2 Process for preparing optically active amino acid derivatives 失效
标题翻译：光学活性氨基酸衍生物的制备方法
公开(公告)号：US06720449B2
公开(公告)日：2004-04-13
申请号：US09926346
申请日：2002-02-05
申请人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
发明人： Masanobu Sugawara , Akio Fujii , Kazumi Okuro , Yasuhiro Saka , Nobuo Nagashima , Kenji Inoue , Toshihiro Takeda , Koichi Kinoshita , Tadashi Moroshima , Yoshihide Fuse , Yasuyoshi Ueda
IPC分类号： C07D20308
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通过N-保护光学活性3-卤代丙氨酸衍生物进行环化生成，或使该衍生物环化，接着进行N-保护，从而得到光学活性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，天然和非天然旋光氨基酸可以是通过简单的程序从便宜的材料生产。

9. 发明申请

US20050228168A1 Method for producing polyhydroxyalkanoate crystal 有权
标题翻译：聚羟基链烷酸酯晶体的制备方法
公开(公告)号：US20050228168A1
公开(公告)日：2005-10-13
申请号：US10992133
申请日：2004-11-19
申请人： Koichi Kinoshita , Fumio Osakada , Yasuyoshi Ueda , Karunakaran Narasimhan , Angella Cearley , Kenneth Yee , Isao Noda
发明人： Koichi Kinoshita , Fumio Osakada , Yasuyoshi Ueda , Karunakaran Narasimhan , Angella Cearley , Kenneth Yee , Isao Noda
IPC分类号： C08F6/00 , C08G63/06 , C08G63/90 , C12P7/62
CPC分类号： C12P7/625 , C08G63/06 , C08G63/90
摘要： The present invention provides a method for conveniently obtaining a biodegradable polyhydroxyalkanoate by a solvent extraction method. A method for producing a polyhydroxyalkanoate crystal comprises precipitating a polyhydroxyalkanoate crystal using a monohydric alcohol having 4 to 10 carbon atoms as a extraction solvent, keeping a polyhydroxyalkanoate solution containing 0.1 to 10% by weight of water relative to the total amount of the solution warm at 70° C. or higher, and cooling the solution to below 70° C.
摘要翻译：本发明提供一种通过溶剂萃取方法方便地获得生物可降解的聚羟基链烷酸酯的方法。聚羟基链烷酸酯晶体的制造方法包括使用具有4〜10个碳原子的一元醇作为提取溶剂使聚羟基链烷酸酯晶体析出，保持含有0.1〜10重量％的水的聚羟基链烷酸酯溶液相对于温度为 70℃以上，将溶液冷却至70℃以下。

10. 发明授权

US06713628B2 Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid 失效
标题翻译：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。

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