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> |