Chemical & Pharmaceutical Bulletin 1989-04-01

Application of dibutyltin oxide method to regioselective acylation and alkylation of tylosin at C-4''.

K Kiyoshima, M Sakamoto, T Ishikura, Y Fukagawa, T Yoshioka, H Naganawa, T Sawa, T Takeuchi

Index: Chem. Pharm. Bull. 37(4) , 861-5, (1989)

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Abstract

4''-O-Acyl-, 4''-O-alkyl- and 4''-deoxy-tylosin derivatives were synthesized using 2'-O-acetyl-3'',4''-O-(dibutyl-stannio)tylosin as a synthetic intermediate. The in vitro biological evaluation showed that the new derivatives were active against macrolide-resistant clinical isolates of bacteria and mycoplasmas, and that they were resistant to hepatic esterase.