发明申请
WO1998043948A1 PROCESS FOR PREPARING O-(3-AMINO-2-HYDROXY-PROPYL)-HYDROXYMIC ACID HALIDES
审中-公开
制备O-(3-氨基-2-羟基丙基) - 羟基酸的方法
- 专利标题: PROCESS FOR PREPARING O-(3-AMINO-2-HYDROXY-PROPYL)-HYDROXYMIC ACID HALIDES
- 专利标题(中): 制备O-(3-氨基-2-羟基丙基) - 羟基酸的方法
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申请号: PCT/HU1997000082申请日: 1997-12-05
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公开(公告)号: WO1998043948A1公开(公告)日: 1998-10-08
- 发明人: BIOREX KUTATO ÉS FEJLESZTO"e; RT.
- 申请人: BIOREX KUTATO ÉS FEJLESZTO"e; RT. , ÜRÖGDI, László , BARABAS, Mihály , MARVANYOS, Ede , TÖRÖK, Magdolna , CSAKAI, Zita
- 专利权人: BIOREX KUTATO ÉS FEJLESZTO"e; RT.,ÜRÖGDI, László,BARABAS, Mihály,MARVANYOS, Ede,TÖRÖK, Magdolna,CSAKAI, Zita
- 当前专利权人: BIOREX KUTATO ÉS FEJLESZTO"e; RT.,ÜRÖGDI, László,BARABAS, Mihály,MARVANYOS, Ede,TÖRÖK, Magdolna,CSAKAI, Zita
- 优先权: HUP 19970403
- 主分类号: C07C249/12
- IPC分类号: C07C249/12
摘要:
The present invention relates to a novel process for preparing O-(3-amino-2-hydroxy-propyl)-hydroxymic acid halides of formula (I) by reacting a carboxamide oxime of formula (II) wherein R is as specified above with reactive 3-amino-2-hydroxy-propane derivative, diazotizing the O-substituted carboxamide oxime thus obtained with sodium nitrite in the presence of hydrogen halide, decomposing the diazonium salt and if desired, separating the optically active enantiomers and/or reacting the resulting base with an organic or mineral acid, wherein the carboxamide oxime of formula (II) is reacted with a 3-hydroxy azetidinium salt of formula (III) wherein R and R are as defined above and Y is a salt forming anion, in a lower alcoholic, preferably ethanolic medium optionally containing water and made alkaline with an alkali hydroxide, and before diazotizing the O-substituted carboxamide oxime intermediate obtained, the reaction mixture is neutralised and the organic solvent is removed. The process according to the invention provides the compounds of formula (I) with a higher yield compared to the prior art processes.