发明公开
- 专利标题: PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE 2-HALOGENO- CARBOXYLIC ACIDS
- 专利标题(中): 工艺制备光学活性2卤代羧酸
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申请号: EP03737476申请日: 2003-02-04
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公开(公告)号: EP1481960A4公开(公告)日: 2005-04-06
- 发明人: YAMASHITA KOKI , TAKEDA TOSHIHIRO , UEDA YASUYOSHI
- 申请人: KANEKA CORP
- 专利权人: KANEKA CORP
- 当前专利权人: KANEKA CORP
- 优先权: JP2002026579 2002-02-04
- 主分类号: C07C51/363
- IPC分类号: C07C51/363 ; C07C51/41 ; C07C51/43 ; C07C51/48 ; C07C51/487 ; 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 1/2 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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