4-N-Acylfortimicin B derivatives and the chemical conversion of fortimicin B to fortimicin A
AssigneeAbbott Laboratories
InventorsJohn S. Tadanier, Jerry R. Martin, Paul Kurath
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Abstract
This invention provides 4-N-acylfortimicin B derivatives of the structure ##STR1## wherein R is acyl, aminoacyl, N-monoloweralkylminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl, or substituted aminoacyl of the formula ##STR2## where R.sup.1 is an acyl radical derived from an amino acid or a short peptide, and the pharmaceutically acceptable salts thereof. The compounds are useful as intermediates for preparing 4-N-alkyl or substituted alkylfortimicin B derivatives. In addition to their utility as intermediates, some of the compounds of this invention are also useful as antimicrobial agents.
Claims3
A method of preparing 1,2',6'-tri-N-benzyloxycarbonyl fortimicin B, which method comprises:
- reacting fortimicin A with N-[benzyloxycarbonyloxy] succinimide to form tetra-N-benzyloxycarbonyl-fortimicin A, and
- hydrolyzing the tetra-N-benzyloxycarbonyl fortimicin A to form said 1,2',6'-tri-N-benzyloxycarbonyl fortimicin B.
Dependencies are inferred from the claim text.