| 摘要 |
NEW MATERIAL:Ailanthone derivatives of formulaIand II (R1 is acryl; R2 is alkene residue of 4-17 carbon atoms). USE:A drug having antitumor activity. PREPARATION:The hydroxyl in the 15 position of 15beta-hydroxy-ailanthone triacylate of formula III is esterified with a residue of an alkene carboxylic acid of 5-18 carbon atoms to give the corresponding 15beta-carboxylic ester of formulaI, or followed by hydrolysis of the product to give a hydroxy compound of formula II. The starting material of formula III is obtained by acylating ailanthone of formula IV, a triterpene occurring in a plant: Ailanthus altissima Swingle in Simaroubaceae, then, subjecting to reduction, dehydration and oxidation to give the compound of formula V and by effecting mild oxidation of the compound of formula V with silver oxide. |
