| 摘要 |
<p>PURPOSE:To obtain a new mycaminosyl tylonolide derivative having a macrocyclic lactone structure, useful as an intermediate for producing 3,4'- dideoxymycaminosyl tylonolide having excellent infection protecting action on Gram-positive and Gram-negative microorganisms. CONSTITUTION:3,2'-Di-O-acetyl-4''-O-isovaleryldemycaminosyl tylosine is mixed with water, an aqueous solution prepared by diluting concentrated sulfuric acid with water is added to the compound while stirring. The compound is dissolved, heated to 50 deg.C and reacted. After the reaction, the reaction solution is cooled to 15 deg.C, washed with ethyl acetate, a water layer is adjusted to pH5.8 with 20% aqueous solution of sodium carbonate, extracted with ethyl acetate and the extracted solution is dried, subjected to dryness under reduced pressure and chromatographed by silica gel thin layer chromatography developed by toluene/acetone (2/1) to give the objective derivative of the formula [R1 is H or OCOCH3; R2 is H or OH protecting group; R3 is acyl; A is (protected) carbonyl; B is (protected) aldehyde; chain line is single bond or double bond; R is lower alkyl, (substituted) aryl, etc.; Me is methyl].</p> |
