| abstract |
NEW MATERIAL:Tylosin derivatives of formula I (R 2 is H, hydroxyl, alkanoyloxy; R 2 is hydroxyl, alkanoyloxy; dotted line means a single or double bond and, when R 1 is H, it is double bond). n EXAMPLE: 3,23-Di-0-acetyl-4'-deoxy mycaminosyl tylonolide. n USE: Antibiotic: they show excellent antibiotic activity and they have a characteristic structure that mycaminosyl thlonolide is made in the deoxy form at the 4' position and simultaneously the 3 and 23 positons are substituted. n PREPARATION: Mycaminosyl tylonolide bearing protected aldehyde in the 18 position of formula II is made to react with benzylsulfonic acid and subsequently with an alkali metal halide to give a halogen-substituted product at the 4' position of formula IV. The dehalogenation at the 4' position is effected to give the deoxy compound of formula V and the protecting group of the aldehyde group is removed to give the compound of formula I. n COPYRIGHT: (C)1982,JPO&Japio |