AMINOGLYCOSIDE ANTIBIOTIC-PROTECTED DERIVATIVE HAVING SELECTIVELY PROTECTED AMINO GROUP EXCEPT AMINO GROUP IN 1-POSITION

摘要

NEW MATERIAL:A compound wherein all the amino group other than amino group in 1,3-positions of aminoglycoside antibiotic having part structure combin ing with a hydroxide group in 6 position of 2-deoxystreptamine with a 3-(alkyl) aminoglycosyl group are protected with an acyl group and amino group in 3'' position is protected with an acyl group expressed by the formula R1CO [R1 is H, 1-6C di(tri)halogenated alkyl] and an amino group in 1-position exists in free form. EXAMPLE:3,6'-Bis(N-benzyloxycarbonyl)-3''-N-trifluoroacetylkanamycin A. USE:A producing raw material for 1-N-(alpha-hydroxy-omega-aminoalkanoyl)-aminogly coside antibiotic. PREPARATION:For example, the aimed compound is obtained by acylating 3'' amino group of 3,6'-bis(N-benzyloxycarbonyl)kanamycin A with an acylating agent such as ethyl trifluoroacetate in a solvent.