发明名称 |
PROCESS FOR PREPARING O-(3-AMINO-2-HYDROXY-PROPYL)-HYDROXYMIC ACID HALIDES |
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 R1 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 R2 and R3 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.
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申请公布号 |
CA2285360(A1) |
申请公布日期 |
1998.10.08 |
申请号 |
CA19972285360 |
申请日期 |
1997.12.05 |
申请人 |
BIOREX KUTATO ES FEJLESZTO RT. |
发明人 |
TOEROEK, MAGDOLNA;MARVANYOS, EDE;UEROEGDI, LASZLO;BARABAS, MIHALY;CSAKAI, ZITA |
分类号 |
C07D295/08;A61K31/15;A61K31/4406;A61K31/444;A61K31/4453;A61K31/4535;A61K31/5375;A61K31/5377;A61P3/10;C07C259/02;C07D213/78;C07D333/40;(IPC1-7):C07C249/12 |
主分类号 |
C07D295/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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