5-Fluorouracil derivatives represented by the formula ##SPC1## Wherein R is arylcarbonyl, substituted arylcarbonyl, heterocyclic carbonyl, alkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, heterocyclic sulfonyl or alicyclic sulfonyl are effective antimetabolites useful in mammary gland or gastrointestinal cancer therapy.
Novel 5-fluorouracil derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrogen atom or methyl group, and R.sub.4 represents a straight or branched alkyl or alkenyl group, which has low toxicity and improved antitumor activity, and novel antitumor preparations containing the said 5-fluorouracil derivative.
The present invention relates to novel N-phthalidyl-5-fluorouracil derivatives represented by the general formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents phthalidyl group ##STR2## (wherein R.sub.3 is a hydrogen atom, a halogen atom or a group selected from alkoxyl groups or alkyl groups) and the other represents a hydrogen atom, an acyl group or a cyclic ether group; ##STR3## (wherein n is 1 or 2) or R.sub.1 and R.sub.2 represent the same phthalidyl group; ##STR4## (wherein R.sub.3 has the same meaning as that defined above) and provides a compound which has antitumor activity and less toxicity and can be used as a cancerocidal agent.
A process is useful for making compounds of the formula: wherein R is hydro, methyl, or fluoro. Valuable intermediates in this process include: ##STR1## wherein R is hydro, methyl, or fluoro, and L is a leaving group.
A method and pesticidal composition for the preventative, protectant, prophylactic and eradicant treatment of plant fungi and bacteria comprises applying an effective amount to plants or seeds of a pesticidal composition containing in an inert carrier a compound of the formula ##STR1## wherein R is hydrogen, methyl or ethyl; R.sup.1 is polyhaloalkyl or polyhalovinyl; R.sup.2 is lower alkyl, lower alkoxy, bromo, chloro, fluoro, lower haloalkyl, cyano, nitro, lower alkylthio, lower alkylcarbonyl, lower alkoxycarbonyl or cycloalkyl; R.sup.3 is hydrogen or independently selected from the values of R.sup.2 ; R.sup.4 is hydrogen or independently selected from the values of R.sup.2 ; X is hydrogen, carbamoyl or cyano; and y is zero, one or two.
