NEW MATERIAL:A 1-carbamoyl-5-fluorouracil derivative expressed by formula I [x is 4-12C alkylene or cycloalkylene: R1 is acyl; R2 is H, 1-13C alkyl, aralkyl, (halogen-substituted)-lower-alkenyl or phenyl which may have a substituent group (lower alkyl, lower alkenyl or halogen); (n) is 0-8].
EXAMPLE: 1-[6-[N-(2-n-Propyl-n-pentanoyl)glycyl]amino-n hexylcarbamoyl]-5- fluorouracil.
USE: An antitumor agent reduced in side effects and having strong antitumor activity.
PREPARATION: 5-Fluorouracil is reacted with phosgene to give 1-chlorocarbonyl 5-fluorouracil expressed by formula II, which is then reacted with a compound expressed by formula V and obtained by subjecting a compound expressed by formula III to condensation through dehydration with a compound expressed by formula IV to provide the compound expressed by formula I.
KITA JUNICHIRO
KAKU YOSHIO
HORIMI IICHIRO