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.
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.
Synthesis and Antitumor Activity of Some Substituted 5-(3-Methyl-4-alkoxybenzyl)pyrimidines.-A variety of new title pyrimidine derivatives [cf. (III), (V), (VI), (VIII), (IX)] are synthesized based on the condensation of malonates (I) with thiourea or guanide. Some of the pyrimidine derivatives obtained display noticeable antitumor activity in addition to low toxicity. -(KALDRIKYAN, M. A.; GRIGORYAN, L. A.; GEBOYAN, V. A.; ARSENYAN, F. G.; STEPANYAN, G. M.; GARIBDZHANYAN, B. T.; Khim. -Farm. Zh. 34 (2000) 10, 9-11; Inst. tonkoi org. khim. im. Mndzhoyana, Nats. Akad. nauk, Erevan 375014, Armenia; RU)
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