PROCESS FOR THE PREPARATION OF AMINOGLYCOSIDE ANTIBIOTICS AND NOVEL INTERMEDIATES THEREFOR

The kanamycin derivatives of formula I, in which R is an amino or hydroxyl group and R is an alkyl group optionally substituted by hydroxyl and/or amino groups, are obtained by alkylation of the compounds of formula II, in which R is H or a benzyl group, R is an acyl-protecting group and R is a hydr...

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Bibliographische Detailangaben
Hauptverfasser:	PLEWS R, MILLION W, RICHARDSON K
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS
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Beschreibung
Zusammenfassung:	The kanamycin derivatives of formula I, in which R is an amino or hydroxyl group and R is an alkyl group optionally substituted by hydroxyl and/or amino groups, are obtained by alkylation of the compounds of formula II, in which R is H or a benzyl group, R is an acyl-protecting group and R is a hydroxyl group or an NHR group, followed by the removal of the R groups and the benzyl group R , where appropriate. The compounds of formula II are new intermediates which are obtained by acylation of a kanamycin A, B or a 3-N-benzylkanamycin A, protected on all its amino functional groups, followed by the removal of the protecting groups and the intramolecular migration of the acyl group from oxygen to nitrogen.