| 摘要 |
NEW MATERIAL:5-Fluorouracil derivatives of formula I [R<1>, R<2> are H, formula H, III (R<3>, R<4> are H, hydroxyl, trialkylsilyloxy, alkoxy, amino, alkoxycarbonylamino, haloalkoxycarbonylamino, nitro, cyano, carboxy, carboxyalkyl; R<5>, R<6> are alkyl); wherein the case where R<1> and R<2> are H at the same time is excluded]. EXAMPLE:1-(3-Oxo-6-cyano-1,3-dihydro-1-isobenzofuranyl)-5-fluorouracil. USE:Antitumor agent: they have high safety and relatively wide range of effective dose, therefore, the dose can be readily increased or decreased and they can be administrered orally or parenterally. PREPARATION:Equimolar amounts or excessive amounts of compounds of formula V and VI (theoretically two equivalent amount is necessary) is made to act on a compound of formula IV, when necessary, hydrolyzed to give the compound of formula I. |
