发明名称 TYLOSIN DERIVATIVE
摘要 <p>NEW MATERIAL:A tylosin derivative shown by the formula I [R1 is alkanoyloxy, (substituted)aromatic acyloxy, tetrahydropyranyloxy, (substituted)benzenesulfonyloxy, etc.; R2 is OH, alkanoyloxy, (substituted) aromatic acyloxy, etc.]. EXAMPLE:3,23-Di-O-acetyl mycaminosyl tylonolide. USE:An antibacterial agent. Having structural characteristics on the point that the titled substance has the substituent groups of R1 and R2 at 23 and 3 positions of mycaminosyl tylonolide. Having more improved antibacterial activity on Gram- negative and Gram-positive Bacteria than tylosin. PROCESS:A compound shown by the formula II [R3 is (protected) aldehyde; R4 is (protected) hydroxyl group] is acylated, and converted into a tetrahydropyranyl compound, etc., to give a compound shown by the formula III (R1' is alkanoyloxy, etc.; R2' is OH, alkanoyloxy, etc.) and the protecting group is removed, to give a compound shown by the formula I.</p>
申请公布号 JPS575000(A) 申请公布日期 1982.01.11
申请号 JP19800079437 申请日期 1980.06.12
申请人 MICROBIAL CHEM RES FOUND 发明人 TANAKA AKIHIRO;TSUCHIYA OSAMU;TAKEUCHI TOMIO;TATSUTA KUNIAKI;SAWA TSUTOMU;TAKAHASHI KOUZOU;ISHIKURA TOMOYUKI;UMEZAWA SUMIO;UMEZAWA HAMAO
分类号 C07H17/08;A61K31/70;A61K31/7042;A61K31/7048;A61P31/04 主分类号 C07H17/08
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