PROCESS AND NOVEL INTERMEDIATES FOR THE PREPARATION OF AMINOGLYCOSIDE ANTIBIOTICS

摘要

The kanamycin derivatives of formula I, in which R is an amino or hydroxyl group and R<1> 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<2> is H or a benzyl group, R<3> is an acyl-protecting group and R<4> is a hydroxyl group or an NHR<3> group, followed by the removal of the R<3> groups and the benzyl group R<2>, 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.