5'-SUBSTITUTED-5-FLUOROURIDINE DERIVATIVE

摘要

NEW MATERIAL:A compound expressed by formula I (R<1> is H, lower alkyl or aralkyl; R<2> is lower alkyl or aralkyl or R<1> and R<2>, together with the adjacent C and O atoms, may form tetrahydrofuranyl or tetrahydropyranyl). EXAMPLE:5'-(Tetrahydropyran-2-yl)-5-fluorouridine. USE:Useful as an antitumor agent having excellent carcinostatic action. PREPARATION:5-Fluorouridine is used as a starting raw material and OH groups at the 2'- and 3'-positions thereof are protected. The resultant compound expressed by formula II (R<3> and R<4> are protecting groups of OH groups) is then reacted with an acetal compound expressed by formula III or enol ether compound expressed by formula IV (R<5> is H, lower alkyl, allyl or aralkyl; R<2> and R<5> may be mutually linked to form dihydropyran or dihydrofuran) in the presence of an acid in a suitable organic solvent to afford a compound expressed by formula V. The protecting groups at the 2'- and 3'-positions are subsequently removed.