Novel 5-fluorouracil derivatives of the following general formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.12 alkanoyl, C.sub.2 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxymethyl, carbamoyl or tri-C.sub.1 -C.sub.5 alkylsilyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.10 aralkyl; X is hydrogen, halogen or C.sub.2 -C.sub.6 alkoxycarbonyl; Y is O, NR' (R' is hy...

A process for producing 5-fluorouracil using an aqueous phosphoric acid solution as a solvent which is a good solvent for an intermediate resulting from the reaction between uracil and elemental fluorine, and permits the reaction to proceed smoothly, but which can precipitate the final product, 5-fluorouracil, after cooling the heat-treated reaction solution to room temperature, with no need to evaporate the solvent. The process comprises reacting uracil in an aqueous phosphoric acid solution wi...

Orally administrable 5-fluorouracil derivatives of the general formula: ##STR1## [wherein R.sup.1 is aryl or substituted aryl; R.sup.2 is acyclic or cyclic alkyl, adamantyl, aryl or substituted aryl; R.sup.3 and R.sup.4 are the same or different, each representing hydrogen atom or lower alkyl] effective against malignant tumors.

This invention relates to a novel 5-fluorouracil derivative represented by the formula ##STR1## wherein R.sup.y is a hydrogen atom or a specific acyl group, Z is a phenyl-lower alkoxy-lower alkyl group, thienyl-lower alkyl group optionally substituted with halogen atom on the thienyl ring, or a group ##STR2## wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a specific acyl group, phenyl-lower alkyl group having a group R.sup.x OCO-- on the phenyl ring, or a group --(A).sub.n B, R.sup.x bein...

Direct fluorination of uracil and its derivatives, in the presence of an aqueous solvent, by fluorine gas to produce 5-fluorouracil and 5-fluorouracil derivatives is disclosed. Novel compounds produced by the reaction, such as 5,5-difluoro-6-hydroxy-5,6-dihydrouracil are also disclosed. The derivatives of 5-fluorouracil are useful as germicidal agents while 5-fluorouracil itself is a known cancer chemotherapy agent.

5-Fluorouracil derivatives and a process for their preparation are provided. The 5-fluorouracil derivatives according to the invention have the general formula: ##STR1## R.sub.1 and R.sub.2 are the same or different and are hydrogen or ##STR2## with the proviso that both R.sub.1 and R.sub.2 are not hydrogen at the same time. A.sub.1, A.sub.2 and A.sub.3 are independently selected from hydrogen, and optionally substituted alkoxy and phenyloxy; at least one of A.sub.1, A.sub.2 and A.sub.3 being ot...

A compound represented by the formulae: ##STR1## wherein R.sub.1 and R.sub.2 are as defined hereinafter, useful as an anti-cancer or anti-tumor agent.

1-Carbamoyl-5-fluorouracil derivatives represented by the formula ##STR1## wherein R.sub.1 represents methyl, ethyl, phenyl or cyclohexyl and R.sub.2 represents hydrogen or is the same as R.sub.1 are effective anti-metabolites useful in treating lymphatic leukemia L1210, sarcoma 180A and Ehrlich ascites carcinoma in mice.

A topical composition comprising LYCD together with known topically active useful medicinal agents such as antiwrinkling, antibiotic, anticancer, antifungal, antiinflammatory such as anti-acne, antiviral, wound healing, and hair-growing agents. The LYCD works together with the other active agents to achieve a synergistic result more effective than can be obtained from the topical agents individually, and more effective than could be predicted from the mere addition of the known efficacies of the...

Homo-oligomeric 5-fluorouridine and 5-fluorodeoxyuridine (FrU.sub.n and FdU.sub.n, n=oligomer length) are synthesized and used as a polymeric drug delivery system for production of FdUMP, the potent inhibitor of thymidylate synthase (TS) and an important target in cancer chemotherapy. Disclosed are methods of both preparing and utilizing said compositions.