Patent ReferencesProcess of selectively blocking amino functions in aminoglycosides using transition metal salts and intermediates used thereby Aminoglycoside antibiotic compounds Production of a selectively protected N-acylated derivative of an aminoglycosidic antibiotic 2-N-Acylated and 2-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides and process 2'-N-Acylated and 2'-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides Patent #: 4468513 InventorsAssigneeApplicationNo. 914451 filed on 10/02/1986US Classes:536/13.7, Kanamycin or derivative536/13.8Carbonyl bonded directly to kanamycin nitrogenExaminersPrimary: Griffin, Ronald W.Assistant: Webber, Pamela S. Attorney, Agent or FirmInternational ClassesC07H 015/20C07H 015/22 Foreign Application Priority Data1985-10-10 ITAbstractA novel process for the synthesis of amikacin starting from kanamycin A protected at the positions 3 and 6' is described comprising the reaction of kanamycin A with a salt of a bivalent metal cation selected from zinc, nickel, iron, cobalt, manganese, copper and cadmium in the presence of water as the solvent or co-solvent followed by the in situ reaction of the resulting complex with a reactive derivative of L-amino-2-hydroxy-butyric acid, removal of the metal cation of the protecting groups and purification of the thus obtained raw product. The acylation under these conditions is extremely selective. |
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