5-Fluorouracil derivatives ⅩⅩⅢ. Synthesis and antitumor activities of 1-carbamoyl-5-fluorouracils having aromatic ring

In order to get good antitumor agents especially better than 5-fluorouracil,tegafur and l-hexylcarbamoyl-5-fluorouracil (HCFU),fourty nine 1-carbamoyl-5-fluorouracil having aromatic ring were synthesized from 5-fluorouracil and isocyanates or amines.Antitumor activity was tested in the L-1210 tumor system,and 5 compounds gave better value of therapeutic ratio than 5-fluorouracil,tegafur,HCFU.l-(4-Methoxybenzylcarbamoyl)-5-fluorouracil gave the best result.