发明申请
- 专利标题: Process for production of optically active 2-halogeno-carboxylic acids
- 专利标题(中): 光学活性2-卤代羧酸的制备方法
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申请号: US10503264申请日: 2003-02-04
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公开(公告)号: US20050176999A1公开(公告)日: 2005-08-11
- 发明人: Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
- 申请人: Koki Yamashita , Toshihiro Takeda , Yasuyoshi Ueda
- 优先权: JP2002-026579 20020204
- 国际申请: PCT/JP03/01092 WO 20030204
- 主分类号: C07C51/363
- IPC分类号: C07C51/363 ; C07C51/41 ; C07C51/43 ; C07C53/15 ; C07C53/16
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.
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