The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jan. 30, 2001
Filed:
Dec. 15, 1999
L{acute over (a)}szl{acute over (o)} {umlaut over (U)}rögdi, Budapest, HU;
Mih{acute over (a)}ly Barab{acute over (a)}s, Budapest, HU;
Ede M{acute over (a)}rv{acute over (a)}nyos, Budapest, HU;
Magdolna Török, M{acute over (a)}t{acute over (e)}szalka, HU;
Zita Cs{acute over (a)}kai, Kunszentmikl{acute over (o)}s, HU;
Biorex Kutato es Fejleszto Rt., Veszprem-Szabadsagpuszta, HU;
Abstract
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 a 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 higher yield compared to the prior art processes.