NEW MATERIAL:The compound of formula {X is H, halogen or methyl; R1 and R2 are H, R3SCO [R3 is (substituted) alkyl, cycloalkyl, aralkyl, aryl, etc.], -CHR5OR4 (R4 and R5 are same as R3), CHR5OCOR4, R5, CONR4R6 (R6 is H or R5), tetrahydrofuryl, phthalidyl or sugar residue; provided that R1≠R2=H}.
EXAMPLE: 1-(Octylthio)carbonyl-5-fluorouracil.
USE: Many compounds of formula exhibit carcinostatic activity and antiviral activity, and can be used for the synthesis of a position-selective substituted pyrimidine compound.
PREPARATION: The compound of formula wherein either one of R1 and R2 is R3SCO and the other is other than H or R3SCO can be prepared by reacting the compound of formula wherein either of R1 and R2 is SCO and H with the compound of formula YCHR5OR4 (Y is halogen), YCHR5OCOR4, YCONR4R6, R5, tetrahydrofuryl halide, phthalidyl halide or a sugar halide.
WATANABE YUTAKA
HOSHIKO TOMONORI
OGASAWARA TOMIO
FUJISAWA HIROSHI
TAKAMI ATSUSHI