| abstract |
NEW MATERIAL:A tylosin derivative shown by the formula I [R 1 is alkanoyloxy, (substituted)aromatic acyloxy, tetrahydropyranyloxy, (substituted)benzenesulfonyloxy, etc.; R 2 is OH, alkanoyloxy, (substituted) aromatic acyloxy, etc.]. n EXAMPLE: 3,23-Di-O-acetyl mycaminosyl tylonolide. n USE: An antibacterial agent. Having structural characteristics on the point that the titled substance has the substituent groups of R 1 and R 2 at 23 and 3 positions of mycaminosyl tylonolide. Having more improved antibacterial activity on Gram- negative and Gram-positive Bacteria than tylosin. n PROCESS: A compound shown by the formula II [R 3 is (protected) aldehyde; R 4 is (protected) hydroxyl group] is acylated, and converted into a tetrahydropyranyl compound, etc., to give a compound shown by the formula III (R 1 ' is alkanoyloxy, etc.; R 2 ' is OH, alkanoyloxy, etc.) and the protecting group is removed, to give a compound shown by the formula I. n COPYRIGHT: (C)1982,JPO&Japio |