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    • 2. 发明申请
    • Process for production of optically active 2-halogeno-carboxylic acids
    • 光学活性2-卤代羧酸的制备方法
    • US20050176999A1
    • 2005-08-11
    • US10503264
    • 2003-02-04
    • Koki YamashitaToshihiro TakedaYasuyoshi Ueda
    • Koki YamashitaToshihiro TakedaYasuyoshi Ueda
    • C07C51/363C07C51/41C07C51/43C07C53/15C07C53/16
    • C07C51/412C07C51/363C07C51/43C07C53/19
    • 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.
    • 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。
    • 5. 发明授权
    • Process for production of optically active 2-halogeno-carboxylic acids
    • 光学活性2-卤代羧酸的制备方法
    • US07473803B2
    • 2009-01-06
    • US10503264
    • 2003-02-04
    • Koki YamashitaToshihiro TakedaYasuyoshi Ueda
    • Koki YamashitaToshihiro TakedaYasuyoshi Ueda
    • C07C53/19C07B39/00
    • C07C51/412C07C51/363C07C51/43C07C53/19
    • 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.
    • 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。
    • 10. 发明授权
    • Processes for producing &bgr;-halogeno-&agr;-amino-carboxylic acids and phenylcysteine derivatives and intermediates thereof
    • 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
    • US06372941B1
    • 2002-04-16
    • US09582461
    • 1999-08-16
    • Koki YamashitaKenji InoueKoichi KinoshitaYasuyoshi UedaHiroshi Murao
    • Koki YamashitaKenji InoueKoichi KinoshitaYasuyoshi UedaHiroshi Murao
    • C07C22900
    • C07C227/16C07C319/14Y02P20/55C07C323/58C07C323/59C07C229/20
    • 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.
    • 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。