Abstract: The compound 6-amino-4-methyl-8-(.beta.-D-ribofuranosyl)pyrrolo[4,3,2-de]pyrimido[4,5-c ]pyridazines-5'-phosphate (a nucleotide) as a new compound and its method of synthesis by phosphorylation of the known 6-amino-4-methyl-8-(.beta.-D-ribofuranosyl)pyrrolo[4,3,2-de]pyrimido[4,5-c ]pyridazine (a nucleoside). The 5'-phosphate ester has utility against L-1210 mouse leukemia and has superior solubility over the parent compound which gives it a broader use pattern relative to dosage. This novel nucleotide also shows advantage in utilization as to pH over, for example, the hydrochloride salt which gives in solution a pH of 4 and is too acid for use.

Abstract: A C-nucleoside compound, 2,4-dichloro-5-(2,3,5-Tri-O-acetyl-.beta.-D-Ribofuranosyl)pyrimidine, useful as a primary starting material in the synthesis of various C-nucleoside compounds having antitumor, antiviral and/or antibacterial activity. A structural formula is as follows: ##STR1## The location of the 2,4-dichloro members on the heterocycle, with the active sites of the carbohydrate being blocked, provides an intermediate compound well adapted for a variety of nucleophilic substitutions. Such procedures have yielded several novel analogs of known pyrimidine nucleosides found in RNA, as well as other compounds which have demonstrated chemotherapeutic utility.

Abstract: 5-ALKYL TRIAZENO URACIL COMPOUNDS AND DERIVATIVES THEREOF WERE SYNTHESIZED BY REACTING AN ALKYL AMINE SUCH AS DIMETHYLAMINE WITH A METHONAL ADDUCT OF 5-DIAZOURACIL AND NUCLEOSIDES THEREOF, UNDER STRINGENT REACTION CONDITIONS TO YIELD THE DESIRED COMPOUNDS. These alkyl triazeno uracil compounds have the structure ##STR1## wherein R is hydrogen or a carbohydrate group, particularly a pentose or hexose monosaccaride such as ribose, arabinose, glucose, and the like, and R' and R" are lower alkyl groups having one to four carbon atoms and wherein R' and R" may be the same or different alkyl groups. The compounds of this invention have been found especially effective as antibacterial and antifungal agents and in inhibiting carcinoma growth in animal tissue.

Abstract: Treatment of the .alpha. and .beta. anomers of 2'-deoxy-6-selenoguanosine with alkyl halides, p-nitrobenzyl bromide, and 5-chloro-1-methyl-4-nitroimidazole under basic conditions has produced the desired products, which are 2'-deoxy-6-R-selenoguanosines where R is the substituent group [2-amino-6-R-seleno-9-(2-deoxy-.alpha.- and .beta.-D-erythro-pentofuranosyl)purines] and R is preferably lower alkyl or aryl. The animal test screening indicated substantial activity for several members of this group of compounds against mouse leukemia L-1210.

Abstract: Novel compounds of the formula ##SPC1##Wherein R is selected from the group consisting of carboxamidine, carboxylic acid, carboxamide, methyl formimidate, thiocarboxamide, carboxamidoxime, carboxamidrazone, and cyano. The compounds have been demonstrated to be useful by having a degree of antimetabolic activity.

Abstract: An improved method for synthesizing 1-(tetrahydro - 2-furanyl) - 5-fluorouracil from a silyl derivitive of 5-fluorouracil (bis - trimethylsilyl 5-fluorouracil) by reacting the same with 2-chlorotetrahydrofuran. The reaction is carried out at controlled conditions of temperature and under an inert gas. Yields in excess of 80% of the theoretical are obtained as calculated upon the starting amounts of 5-fluorouracil.

Abstract: A facile process for the production of Ftorafur [1-(tetrahydro-2-furanyl)-5-fluorouracil] which comprises reacting 2,4-bis-trimethylsilyl uracil with 2-chlorotetrahydrofuran to produce 1-tetrahydro-2-furanyluracil at low temperatures in a dry non-aqueous solvent, e.g. a halogenated hydrocarbon solvent such as methylene chloride. Subsequently the desired final product is produced by direct fluorination of the uracil ring as the last step utilizing a fluorinating agent such as trifluoromethylhypofluorite. This step is conducted in the cold and again in the presence of a halogenated hydrocarbon solvent such as chloroform. Ftorafur has been utilized as a pyrimidine analog for the management of carcinoma in the breast and large intestine and with less side effects than 5-fluorouracil (5-FU).