Synthesis of nucleoside - 3 - substituted 1,2,4-triazole

摘要

1-(O-acyl-blocked-ss-D-ribofuranosyl)-1,2,4-triazoles which are substituted in position 3 and have the formula I IMAGE where Ac and Y have the meaning stated in Claim 1 are prepared by reacting corresponding triazoles with corresponding ribofuranone derivatives. The acyl groups can be eliminated by hydrolysis from the compounds of the formula I according to the invention. The hydrolysed products can in turn be used to prepare corresponding phosphorylated compounds of the general formula V IMAGE in which Y has the same meaning as in formula I, and at least one of the Z radicals has the meaning of an acyl group of phosphoric acid while the other Z radical either likewise has the meaning of an acyl radical of phosphoric acid or is a hydrogen atom. The hydrolysed products are then esterified to give the phosphoric esters of the formula V. The compounds of the formula I, as well as the 1-(ss-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide-nucleosides obtained on hydrolysis thereof, display both a considerable antiviral activity and an antitumour activity.