Icn Pharmaceuticals, Inc.

Leon F Christensen

Roland K Robins

Joseph T Witkowski

1-.beta.-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide is prepared by a process wherein a suitably substituted formimidic acid hydrazide is condensed with a blocked derivative of D-ribose and the intermediate is ring closed with a reagent which donates one carbon atom to yield a 3-substituted-1-(blocked .beta.-D-ribofuranosyl)-1,2,4-triazole. Treatment of this intermediate with ammonia and/or removal of the blocking group yields the product.

Process for preparing 1,2,4-triazole nucleosides

Novel compounds of the general formula ##SPC1## Wherein X is H or NH.sub.2 ; R' is C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.8 substituted alkyl, benzyl, C.sub.1 to C.sub.8 acyl, benzoyl, carbamoyl, are disclosed as well as a novel free radial alkylation and acylation process for making such compounds. The compounds of the invention display activity comparable to or superior to their naturally occurring analogue while resisting phosphodiesterase degradation. In some cases the compounds of this invention actually inhibit enzymatic degradation of the natural analogue.

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Costa Mesa, CA, United States of America

Leon F Christensen