ANALOGIFREMGANGSMAADE TIL FREMSTILLING AF 1N-(ALFA-HYDROXY-OMEGA-AMINOALKANOYL)-6'N-METHYL-3',4'-DIDEOXYKANAMYCIN B

摘要

1-N-(alpha-hydroxy-omega-aminoalkanoyl)-6'-N-methyl-3',4'-dideoxyka namycins B or pharmaceutically acceptable acid addition salts thereof are prepared by selective acylation of the 1-amino group of an amino-protected derivative of the formula in which R1 is a monovalent amino protective group and R2 is hydrogen or a monovalent amino protective group, with an alpha -hydroxyomega -amino acid of the formula V or with a functional derivative thereof, in which n is 1, 2 or 3, R3 is an amino protective group and R4 is hydrogen, or R3 and R4 together are a divalent amino protective group, after which the amino protective groups are eliminated from the 1-N-acylated product obtained in this way. The prepared compounds are effective not only against Gram-negative and Gram-positive bacteria with the usual kanamycin sensitivity but also against kanamycin-resistant bacteria.