Novel compounds comprising 5-fluorouracil or 5-fluorouridine covalently linked to 5-ethynyluracil, 5-ethynyluridine or 5-propynyluracil and pharmaceutical compositions comprising such compounds are disclosed.

Oil-in-water emulsion formulations contain both free fluorouracil and fluorouracil impregnated in porous microparticles. The formulations are suitable for topical administration, and are useful for the treatment of solar keratoses, actinic keratoses, and superficial basal cell carcinomas.

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.

An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be...

A method of producing 5-fluorouracil which includes the fluorination of uracil with elementary fluorine diluted with an inert gas in a glacial acetic acid medium under hydrodynamic conditions of Re=35,000-45,000 at a temperature of from 15.degree. to 35.degree. until the uracil disappears from the reaction mixture, whereafter said mixture is heated at a temperature of from 90.degree. to 95.degree.C until 5-fluoro-6-acetoxy-dihydrouracil formed during the fluorination disappears therefrom, follow...

A homo-oligonucleotide of between 2 and 26 monomers of 5-fluorouridine 5'-monophosphate or 5-fluorodeoxyuridine 5'-monophosphate covalently linked via 3'- to 5'-phosphodiester linkages, where at the 3'- or 5'- terminus there is covalently linked a molecule selected from the group consisting of cholesterol, ethyl-spaced adamatane, 1,2-di-hexadecylglycerol and poly-L-lysine. These homo-oligonucleotides exhibit antitumor activity.

The present invention concerns the method for producing 5-fluorouracil. In accordance with the said method uracil is brought to interact with fluorine in diluent medium which partly or completely dissolves uracil without interacting with fluorine, in an atmosphere of inert gas with subsequent separation of the formed end product. It is preferable to employ acetic acid as diluent, and nitrogen as the inert gas. The end product 5-fluorouracil finds wide application in cancer therapy of the mammary...

An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be...

5-Fluorouraacil is produced by reacting orotic acid with a fluorinating agent and then, decarboxylating the resulting 5-fluoro-orotic acid.

A process for preparing 5-fluorouracil, and a novel starting compound for such process, are disclosed. The novel starting compound is 2,4,5-trifluoropyrimidine. The process comprises hydrolyzing the 2,4,5-trifluoropyrimidine at a temperature of about 2.degree. to about 100.degree. C., thereby directly producing the compound 5-fluorouracil. 5-Fluorouracil is a known anti-tumor agent, which has been used in the treatment of various types of cancers. In addition, 5-fluorouracil is a starting materi...