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1. 发明授权

US07057066B2 Process for producing 3-amino-2-hydroxypropionic acid derivatives 失效
标题翻译： 3-氨基-2-羟基丙酸衍生物的制备方法
公开(公告)号：US07057066B2
公开(公告)日：2006-06-06
申请号：US10312208
申请日：2001-06-26
申请人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C229/06 , C07C229/34
CPC分类号： C07D263/20 , C07C227/20 , C07C227/32 , C07C227/42 , Y02P20/55 , C07C229/22 , C07C229/34
摘要： The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).
摘要翻译：本发明提供了一种制备不使用危险试剂的3-氨基-2-羟基丙酸衍生物（1）的方法，在经济上是有利的，适用于工业生产，该方法包括：将N-保护的3- 具有与衍生物（1）相反的2-位碳位置的氨基-2-羟基丙酸衍生物（2）与离去基团引入剂转化为N-保护的3-氨基丙酸衍生物（3），然后用碱性物质处理衍生物，将其转化成在2-位碳上具有反向立体构型的取代-3-氨基-2-羟基丙酸衍生物（4），然后将其转化为3-氨基-2-羟基丙酸衍生物（1）。

2. 发明申请

US20050176999A1 Process for production of optically active 2-halogeno-carboxylic acids 失效
标题翻译：光学活性2-卤代羧酸的制备方法
公开(公告)号：US20050176999A1
公开(公告)日：2005-08-11
申请号：US10503264
申请日：2003-02-04
申请人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C51/363 , C07C51/41 , C07C51/43 , C07C53/15 , C07C53/16
CPC分类号： C07C51/412 , C07C51/363 , C07C51/43 , C07C53/19
摘要： The invention provides processes for producing efficiently optically active 2-halogenocarboxylic acids useful in the preparation of drugs or the like and salts thereof with amines. Specifically an optically active 2-halogenocarboxylic acid is produced by halogenating an optically active amino acid in water in the presence of a hydrophobic organic solvent and nitrous acid with the configuration retained and with the racemization inhibited through the removal of 2-hydroxy-bromocarboxylic acid formed as a by-product; the obtained optically active 2-halogenocarboxylic acid is transferred to an aqueous phase by converting it into a salt thereof with a base, followed by the removal of the organic phase; and the optically active 2-halogenocarboxylic acid is transferred again to an organic solvent phase, followed by the removal of the aqueous phase, whereby an optically active 2-halogenocarboxylic acid is obtained through the removal of a halogen component. Further, a high-quality salt of an optically active 2-halogenocarboxylic acid with an amine can be obtained by a crystallization method wherein the amine is added over the period of ½ hour or longer either continuously or in portions and/or wherein the crystallization solvent consists of a hydrophobic organic solvent and a hydrophilic organic solvent.
摘要翻译：本发明提供了可用于制备药物等的有效光学活性2-卤代羧酸的方法及其与胺的盐。具体地说，光学活性的2-卤代羧酸是通过在疏水性有机溶剂和亚硝酸存在下在水中卤化光学活性氨基酸而形成的，其中保留了结构，并且通过除去形成的2-羟基 - 溴代羧酸来抑制外消旋化作为副产品; 将得到的光学活性2-卤代羧酸通过将其转化为其盐与碱反应，然后除去有机相，转移到水相中。并将光学活性2-卤代羧酸再次转移到有机溶剂相中，然后除去水相，由此通过除去卤素组分获得光学活性的2-卤代羧酸。此外，光学活性2-卤代羧酸与胺的高品质盐可以通过结晶方法获得，其中胺在连续或部分加入0.5小时或更久的时间内和/或其中结晶溶剂由疏水性有机溶剂和亲水性有机溶剂构成。

3. 发明授权

US07307184B2 Processes for preparing oxazolidinone derivatives of β-hydroxyethlamine compounds and for preparing β-hydroxyethlamine compounds 失效
标题翻译：制备β-羟基三甲基胺化合物的恶唑烷酮衍生物和制备β-羟基三甲基胺化合物的方法
公开(公告)号：US07307184B2
公开(公告)日：2007-12-11
申请号：US10478439
申请日：2002-05-23
申请人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi Murao , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C269/00 , C07C269/06
CPC分类号： C07D263/24 , C07D263/22
摘要： The present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare oxazolidinone derivatives of β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises introducing a step of treating in contact with water with heating under acidic to neutral conditions into the process. Also, the present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises subjecting the oxazolidinone derivatives prepared as described above to a step of treating in contact with water under basic conditions.
摘要翻译：本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备β-位羟基化合物的恶唑烷酮衍生物的方法，所述β-羟乙基胺化合物在β-位置碳具有反向立体构型，其包括引入步骤在酸性到中性条件下加热处理与水接触。此外，本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备在β-位置碳具有反向立体构型的β-羟乙基胺化合物的方法，该方法包括使恶唑烷酮衍生物如上所述制备成在碱性条件下与水接触的步骤。

4. 发明申请

US20060135784A1 PROCESS FOR PRODUCING 3-AMINO-2-HYDROXYPROPIONIC ACID DERIVATIVES 审中-公开
标题翻译：生产3-氨基-2-羟基丙酸衍生物的方法
公开(公告)号：US20060135784A1
公开(公告)日：2006-06-22
申请号：US11276222
申请日：2006-02-17
申请人： Hiroshi MURAO , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Hiroshi MURAO , Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07D263/38 , C07D263/04
CPC分类号： C07D263/20 , C07C227/20 , C07C227/32 , C07C227/42 , Y02P20/55 , C07C229/22 , C07C229/34
摘要： The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).
摘要翻译：本发明提供了一种制备不使用危险试剂的3-氨基-2-羟基丙酸衍生物（1）的方法，在经济上是有利的，适用于工业生产，该方法包括：将N-保护的3- 具有与衍生物（1）相反的2-位碳位置的氨基-2-羟基丙酸衍生物（2）与离去基团引入剂转化为N-保护的3-氨基丙酸衍生物（3），然后用碱性物质处理衍生物，将其转化成在2-位碳上具有反向立体构型的取代-3-氨基-2-羟基丙酸衍生物（4），然后将其转化为3-氨基-2-羟基丙酸衍生物（1）。

5. 发明授权

US07473803B2 Process for production of optically active 2-halogeno-carboxylic acids 失效
标题翻译：光学活性2-卤代羧酸的制备方法
公开(公告)号：US07473803B2
公开(公告)日：2009-01-06
申请号：US10503264
申请日：2003-02-04
申请人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
发明人： Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
IPC分类号： C07C53/19 , C07B39/00
CPC分类号： C07C51/412 , C07C51/363 , C07C51/43 , C07C53/19
摘要： The invention provides processes for producing efficiently optically active 2-halogenocarboxylic acids useful in the preparation of drugs or the like and salts thereof with amines. Specifically, an optically active 2-halogenocarboxylic acid is produced by halogenating an optically active amino acid in water in the presence of a hydrophobic organic solvent and nitrous acid with the configuration retained and with the racemization inhibited through the removal of 2-hydroxy-bromocarboxylic acid formed as a by-product; the obtained optically active 2-halogenocarboxylic acid is transferred to an aqueous phase by converting it into a salt thereof with a base, followed by the removal of the organic phase; and the optically active 2-halogenocarboxylic acid is transferred again to an organic solvent phase, followed by the removal of the aqueous phase, whereby an optically active 2-halogenocarboxylic acid is obtained through the removal of a halogen component. Further, a high-quality salt of an optically active 2-halogenocarboxylic acid with an amine can be obtained by a crystallization method wherein the amine is added over the period of ½ hour or longer either continuously or in portions and/or wherein the crystallization solvent consists of a hydrophobic organic solvent and a hydrophilic organic solvent.
摘要翻译：本发明提供了可用于制备药物等的有效光学活性2-卤代羧酸的方法及其与胺的盐。具体地说，光学活性2-卤代羧酸是通过在疏水性有机溶剂和亚硝酸的存在下在水中卤化光学活性氨基酸而形成的，其中保留了结构，并且通过除去2-羟基 - 溴羧酸，外消旋化被抑制形成副产品; 将得到的光学活性2-卤代羧酸通过将其转化为其盐与碱反应，然后除去有机相，转移到水相中。并将光学活性2-卤代羧酸再次转移到有机溶剂相中，然后除去水相，由此通过除去卤素组分获得光学活性的2-卤代羧酸。此外，光学活性2-卤代羧酸与胺的高品质盐可以通过结晶方法获得，其中胺在连续或部分加入0.5小时或更久的时间内和/或其中结晶溶剂由疏水性有机溶剂和亲水性有机溶剂构成。

6. 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。

7. 发明申请

US20050118288A1 Method for producing high-quality hydropbic licorice extract 审中-公开
标题翻译：生产高品质Hydropbic甘草提取物的方法
公开(公告)号：US20050118288A1
公开(公告)日：2005-06-02
申请号：US10504256
申请日：2003-02-20
申请人： Koki Yamashita , Tadao Ono , Shiro Kitamura , Yasuyoshi Ueda
发明人： Koki Yamashita , Tadao Ono , Shiro Kitamura , Yasuyoshi Ueda
IPC分类号： A23K1/14 , A23K1/16 , A23L1/236 , A23L1/30 , A61K9/20 , A61K31/352 , A61K31/37 , A61K31/56 , A61K36/484 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P43/00 , C07J63/00 , A61K35/78
CPC分类号： C07J63/00 , A23K10/30 , A23K20/10 , A23L27/30 , A23L33/105 , A23V2002/00 , A61K31/352 , A61K31/37 , A61K31/56 , A61K36/484 , A23V2250/252
摘要： It is an object of the present invention to provide a method for producing a hydrophobic licorice extract which is useful for applications, such as food, food additives, functional nutritive food, food for specified health uses, dietary supplements, drink, feedstuff, drugs, and quasi-drugs, and which has satisfactory powder characteristics. This invention relates to a method for producing a hydrophobic licorice extract comprises performing extraction from licorice with a water-soluble organic solvent, the area of the bark of the licorice occupying at least 30% of the total surface area of the licorice. This invention also relates to a method for producing a hydrophobic licorice extract comprises crystallizing an extract extracted from licorice, or an extraction residue of the licorice, with a water-soluble organic solvent in a mixed solvent comprising water and the water-soluble organic solvent, the weight ratio, water/(water-soluble organic solvent+water), being ⅓ or more.
摘要翻译：本发明的目的是提供一种制备疏水性甘草提取物的方法，其可用于食品，食品添加剂，功能性营养食品，特定健康用途食品，膳食补充剂，饮料，饲料，药物，和准药，具有令人满意的粉末特性。本发明涉及一种生产疏水甘草提取物的方法，包括用水溶性有机溶剂从甘草中提取甘草的皮肤面积占甘草总表面积的至少30％。本发明还涉及一种疏水性甘草提取物的制造方法，其特征在于，包括使水溶性有机溶剂在水和水溶性有机溶剂的混合溶剂中结晶从甘草提取的提取物或甘草的提取残渣，重量比，水/（水溶性有机溶剂+水）为1/3以上。

8. 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。

9. 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）。

10. 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。

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