No abstract

A series of 3-benzofuryl-4-phenyl(allyl)-5-mercapto-1,2,4-triazoles have been synthesized by cyclization of the corresponding substituted thiosemicarbazides of benzofuran-2-carboxylic acid. S-alkylation of 5-mercaptotriazoles with various alkyl-, alkenyl-, and benzyl-substituted benzyl chlorides; chloroacetamides; and chloroacetic-, 2-bromopropionic-, and 2-bromocaproic acids has been studied. The antitumor activity of the synthesized compounds was tested.

Conditions for effective alkylation of new 3,4-substituted-5-mercapto-1,2,4-triazoles with various alkylating agents are established. Several compounds possessing pronounced antitumor activity have been found in experiments using two xenograft tumor models.

New 2-S-4,5,6-substituted pyrimidines have been prepared via the reaction of 2-mercaptopyrimidines with allyl-, methallyl-, and substituted-benzyl chlorides, chloroacetamide, and chloracetic, á-bromopropionic, and á-bromocaproic acids. Reactions of 2-methylthio-derivatives with morpholine, piperidine, and o-and p-anisidines yielded the corresponding 2-amino-derivatives. The antitumor properties of the synthesized compounds have been studied.

S‐Fluoruracil (I) wird mit Benzylchloriden (IIa)‐(IIe) alkyliert.