1-N-((S)-{60 -substituted-{107 -aminoacyl)-neamine or -ribostamycin and the production thereof

摘要

An 1-N-((S)- alpha -substituted- omega -aminoacyl)-neamine or -ribostamycin of the formula: <IMAGE> wherein R is a hydrogen atom or beta -D-ribofuranosyl group of the formula <IMAGE> and R3 is hydroxyl, amino-NH2 or acylamino group -NHR4 in which R4 is an acyl group, and n is a whole number of 1 to 4, may be produced by subjecting the corresponding O-((S)- alpha -substituted- omega -aminoacyl)-neamine or -ribostamycin of the formula <IMAGE> or its hydroxyl-masked and amino-masked form, to the action of a basic medium to produce an acyl-migration product of the formula: <IMAGE> and, optionally converting the amino-masking groups into hydrogen atoms and also the hydroxyl-masking group into hydrogen atom in a known manner if said amino-masking groups and said hydroxyl-masking groups are present in the acyl-migration product. The 1-N-((S)- alpha -substituted- omega -aminoacyl)-neamine or -ribostamycin produced is characterized by its useful activity inhibitory to the growth of bacteria resistant to the parent substance neamine or ribostamycin.