| 摘要 |
NEW MATERIAL:The 5-fluorouracil derivative of formula (R is acyl derived from triene higher fatty acid or pentaene higher fatty acid). EXAMPLE:1-(alpha-Linoleylaminomethylcarbamoyl)-5-fluorouracil. USE:A carcinostatic agent and platelet coagulation inhibitor. PREPARATION:The objective compound of formula is produced by reacting 5-fluorouracil (5-FU) with the compound of formula R-NHCH2CO2H in a solvent such as dimethylformamide, dioxane, etc., in the presence of diphenylphos phorylazide. The compound exhibits an antitumor activity (carcinostatic activity) comparable to or higher than 5-FU, and has lower toxicity than 5-FU. It has strong platelet coagulation inhibiting activity which cannot be found in 5-FU. It is administered in a dose of preferably about 1-3g daily for adults.
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