Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.

Abstract: 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 material for the production of certain types of pro-drugs, which are metabolized to form 5-fluorouracil in the body, such as, for instance, the compound 1-(2-tetrahydrofuryl)-5-fluorouracil.

Abstract: Novel orotic acid derivatives useful as agricultural chemicals or intermediates thereof are disclosed. The orotic acid derivatives are represented by the formula ##STR1## where Me is an alkali metal, R.sup.1 is an alkyl group of from 1 to 4 carbon atoms, an allyl group, a cyclohexyl group, a benzyl group, or a group ##STR2## (where R.sup.2 is an alkyl group of from 1 to 4 carbon atoms, an alkoxyl group of from 1 to 4 carbon atoms or a halogen atom and n is 0, 1, 2 or 3), m is an integer of 1 or 2, and X is a chlorine, bromine or iodine atom or a group --COR.sup.0 (where R.sup.0 is an alkyl group of from 1 to 4 carbon atoms or a phenyl group) when m is 1, and a group --COO.sup.- when m is 2.

Abstract: There is provided a method for the treatment of viral infections by treating a host animal with a pharmaceutically effective amount of a carbocyclic analog of a nucleoside represented by Formula I: ##STR1## wherein X is chlorine, bromine, iodine, a lower alkyl group or an amino group of the formula --NHR.sup.2 wherein R.sup.2 is a lower alkyl group; and R and R' can be the same or different members selected from the group consisting of hydrogen, an alkanoyl group or an aroyl group.

Abstract: Novel derivatives of pyrimid-2-one having interesting pharmacological properties are described. The compounds of the invention have been found to be of use in the control of, and in particular in the inhibition of the metaphase of malignant tumours and leukaemias. Processes for the preparation of the novel compounds and pharmaceutical compositions containing them are also described.

Abstract: A compound of the formula: ##STR1## wherein R is a bridged alicyclic group selected from the group consisting of norbornyl, norbornenyl, bicyclo[2,2,2]-heptyl and adamantyl optionally substituted by at least one substituent selected from the group consisting of lower alkyl, carboxy, lower alkoxycarbonyl, alkylidenedioxy, N,N-di(lower)alkylcarbamoyl, amino, loweralkoxycarbonylamino and halogen. The present compound is useful in the therapeutic treatment of cancer in human beings and animals.

Abstract: Nucleoside analogues having a ring-open structure, of general formula: ##STR1## where R and R' may be hydrogen, silyl groups, substituted alkyl groups and the like, and B is a base such as adenine, have been shown to exhibit anti-viral and other biological activities at non-toxic levels. Also provided are phosphate-linked dinucleotide compounds of similar structures.

Abstract: 4-Ethyl-6-methoxy-7-(oxiranylmethoxy)quinazoline and its isomer 4-ethyl-7-methoxy-6-(oxiranylmethoxy)quinazoline have potent anti-tumor activity in animals.

Abstract: 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.

Abstract: The present invention relates to a novel process for producing pyrimidine nucleosides by a reaction between bis(tri-lower alkylstannyl)-5-halogenouracil and 2-substituted tetrahydrofurane. The novel process of the present invention makes it possible to obtain, depending upon the manner of substitution of tetrahydrofurane residue on two nitrogen atoms N.sub.1 and N.sub.3 of 5-halogenouracil, N.sub.1 -mono-substituted compound, N.sub.3 -mono-substituted compound and N.sub.1,N-di-substituted compound among which the last can be converted by hydrolysis thereof into N.sub.1 -mono-substituted compound. The present invention further relates to novel N.sub.3 -mono-substituted compounds and N.sub.1,N.sub.3 -di-substituted compounds obtained by such process. The present invention still further relates to novel bis-(tri-lower alkylstannyl)-5-halogenouracil used in the present invention as a raw compound.

Abstract: 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 material for the production of certain types of pro-drugs, which are metabolized to form 5-fluorouracil in the body, such as, for instance, the compound 1-(2-tetrahydrofuryl)-5-fluorouracil.

Abstract: New uracil derivatives of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom or a grouping of the formula: ##STR2## R.sup.2 for a hydrogen atom, an alkyl group or a phenyl group and R.sup.3 for an alkyl group or a phenyl group, with the proviso that when both R.sup.1 and R.sup.2 stand for a hydrogen atom, R.sup.3 stands for a phenyl group or a straight chain alkyl group with 3.about.11 carbon atoms, that when R.sup.1 stands for a hydrogen atom and R.sup.2 for methyl group, R.sup.3 stands for an alkyl group with at least 2 carbon atoms or a phenyl group, and that when R.sup.1 stands for a hydrogen atom and R.sup.3 for methyl group, R.sup.2 stands for an alkyl group with at least 2 carbon atoms or a phenyl group. These uracil derivatives are prepared by reacting 5-fluorouracil with an .alpha.-haloalkyl carboxylate or with an aldehyde diacylate or by hydrolyzing a 1,3-bis(acyloxymethyl)-5-fluorouracil with an acid or alkali.

Abstract: A process for efficiently preparing 1-(2-tetrahydrofuryl)-5-fluorouracil useful as an antitumor agent or an antiviral agent which comprises reacting 5-fluorouracil with 2,3-dihydrofuran. This reaction proceeds advantageously in the presence of a reaction accelerator such as a Lewis acid in a polar solvent such as pyridine.

Abstract: A new and industrially useful method of producing 1(or 1,3-bis)-(tetrahydro-2-furyl)-5-fluorouracil or a mixture thereof by reacting 5-fluorouracil with 2,3-dihydrofuran at elevated temperature in a closed vessel. Depending upon reaction conditions, each of the above 5-fluorouracil derivatives or a mixture of them is produced.1,3-Bis-(tetrahydro-2-furyl)-5-fluorouracil thus formed can be converted to 1-(tetrahydro-2-furyl)-5-fluorouracil by solvolysis under non-acidic conditions.

Abstract: Direct fluorination of uracil, cytosine and their derivatives, in the presence of a non-aqueous solvent, by fluorine gas to produce 5-fluorouracil, 5-fluorocytosine, 5-fluorouracil derivatives and 5-fluorocytosine derivatives is disclosed. The non-aqueous solvent is an acid or alcohol, which can be partly or fully fluorinated or chlorinated, of up to 8 carbon atoms, such as trifluoroacetic acid. Novel compounds produced by the reaction, such as 5,5-difluoro-5,6-dihydro-6-(2,2,2-trifluoroethoxy) uracil are also disclosed. The derivatives and 5-fluorocytosine are useful as germicidal and antineoplastic agents while 5-fluorouracil itself is a known cancer chemotherapy agent.

Abstract: Carcinostatic composition containing an oily substance such as a glyceride and 3-N-o-toluyl-5-fluorouracil suspended therein. The composition exhibits a remarkable carcinostatic effect against various cancerous cells at a low dose and has less side-effects than 5-fluorouracil and its known derivatives which have been typical carcinostatic compounds. A process of producing carcinostatic composition comprises dispersing 1,3-di-N-acyl-5-fluorouracil into an oily substance such as a glyceride to prepare an emulsion and selectively substituting a hydrogen atom only for the 1-position acyl group, whereby the compound is acylated only at the 3-position and which is a chief constituent of the carcionstatic composition.

Abstract: Ethylenically unsaturated compositions such as acrylic and methacrylic acid esters, vinyl esters, vinyl halides, unsaturated amides such as acrylamide, vinyl aromatics such as styrene, and various aliphatic and aromatic polyesters containing any of the above or other modifying components such as maleic, fumaric, itaconic, citraconic and the like, are very effectively and rapidly cured with certain 5-halo-6-halomethyluracil photoinitiators. These curable systems have extensive utility in the surface coatings industry, particularly in regard to cured protective coatings.

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

Abstract: The present invention relates to a new process for the preparation of N.sup.1 -(2'-furanidyl)-5-fluoro-uracil, also called Ftorafur, which is a very important anti-cancer compound. Said process comprises reacting 2,3-dihydrofuran with water in the presence of a catalytic amount of an acidic catalyst at a pH below 2.5, removing excess of unreacted starting materials and reacting the mixture obtained with silylated-5-fluoro-uracil is in the presence of a Friedel Crafts type catalyst uracil in an inert organic solvent. The new process has many advantages in comparison with those used so far.

Abstract: The present disclosure relates to a compound of the general formula: ##STR1## and the novel antipodes of that compound.

Abstract: A novel and very elegant method is proposed for the preparation of N.sub.1 -(2-tetrahydrofuryl)-5-substituted or -unsubstituted uracil, especially, N.sub.1 -(2-tetrahydrofuryl)-5-fluorouracil, by the reaction of the corresponding 5-substituted uracil compound with 2,3-dihydrofuran. The reaction is performed in the presence of a chlorosilane compound, e.g. dimethyldichlorosilane, and a catalytic amount of an organic amine compound and can proceed very rapidly without disadvantageous side reactions to give the objective compound with high purity in a high yield.

Abstract: Isoxazolo[3,4-d]pyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 respectively, are hydrogen, lower alkyl, cycloalkyl, or aryl which may be substituted by halogen, are useful as antiinflammatory-analgesic drugs, and the industrially feasible production thereof is provided.

Abstract: 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 other than hydrogen. The 5-fluorouracil derivative is prepared by condensing 5-fluorouracil with a halide of the formula: ##STR3## in the presence of a base. The 5-fluorouracils according to the invention show anti-tumor activity.

Abstract: A process for production of 5-fluorouracil and its derivatives which comprises reacting a cytosine compound of the formula: ##STR1## wherein R is a hydrogen atom or a saccharide residue with fluorine or fluorine fluorosulfonate (FOSO.sub.2 F) in an aqueous medium to give the corresponding 5-fluorouracil compound of the formula: ##STR2## wherein R is as defined above.

Abstract: 5-Fluorouracil derivative having the formula ##STR1## wherein R represents hydrogen atom or 2-tetrahydrofuryl group is produced by reacting more than equi-mole of 2,3-dihydrofuran with 5-fluorouracil in a polar aprotic solvent with a catalytically effective amount of a catalyst selected from the group consisting of metal halides, non-metal halides, tertiary amine salt of inorganic acids and organic acids in neutral or basic condition at 50.degree. to 150.degree. C under pressure.

Abstract: N.sup.1 -(2-tetrahydrofuryl)-5-fluorouracil is produced in high yield by reacting 5-fluorouracil with 2,3-dihydrofuran in the presence of trimethylsilyl chloride and a tertiary amine and treating the resultant mixture with an aqueous alkaline solution.

Abstract: Process for preparing N.sub.1 -(2'-furanidyl)-5-fluorouracil having effective pharmacological activities such as anti-leukemia and anti-tumor activities comprising reacting 2,4-bis(trialkylsilyl)-5-fluorouracil with 2,3-dihydrofuran in the presence of a proton donor and a catalyst. Such process can be simply, easily conducted to give the desired product having a high purity in good yield.

Abstract: A 5-fluoropyrimidin-4-one derivative represented by the formula ##STR1## wherein R is straight-chain or branched-chain alkyl having 4 to 18 carbon atoms, straight-chain or branched-chain alkenyl having 2 to 18 carbon atoms, alkylene oxido having 3 to 10 carbon atoms, aryl or aralkyl;Processes for preparing the derivative;An anti-tumor composition containing the derivative as an effective component and an excipient.

Abstract: 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.