2-Hydroxy gentamicin compounds
AssigneeSterling Drug Inc.
InventorsHaruo Yamamoto, Sol J. Daum
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Abstract
2-Hydroxygentamicins B, B.sub.1 and A.sub.3 and 2-hydroxy antibiotics JI-20A and JI-20B are prepared as fermentation products by culturing a nutrient medium containing carbohydrates, a source of assimilable nitrogen, essential salts and D-streptamine with a mutant of Micromonospora purpurea, and isolating the said fermentation products from the nutrient medium; the fermentation products are acylated with an ester of an .omega.-(N-benzyloxycarbonyl)amino-.alpha.-hydroxy-lower-alkanoic acid, after first blocking the 6'-and/or 2'-amine group with an amine-protecting group, followed by catalytic hydrogenolysis of the benzyloxycarbonyl group and removal of the amine-protecting groups to prepare the 1-N-(.omega.-amino-.alpha.-hydroxy-lower-alkanoyl) derivatives.
Claims6
A member of the group consisting of (A) a compound having one of the formulas:
- ##STR4## where R.sub.1 is hydrogen or an .omega.-amino-.alpha.-hydroxy-lower-alkanoyl group, H.sub.2 N(CH.sub.2).sub.n CHOHCO-, where n is one of the integers 1 or 2;
- and where, in formula Ia, R.sub.2 ' is hydroxy or amino and R.sub.6 ' is hydrogen or methyl;
- and (B) acid-addition salts thereof.
Dependencies are inferred from the claim text.