1,2,4-triazole nucleosides
Abstract
Abstract AS ANTIVIRAL AGENTS AND INTERMEDIATES THEREFOR, 3-SUBSTITUTED 1-(B-D-GLYCOSYL)-1,2,4-TRIAZOLES, O-ACYLATED ANALOGS THEREOF, AND 5''- AND 3'',5''-CYCLIC PHOSPHATES OF THE TRIAZOLE NUCLEOSIDES, "GLYCOSYL" BEING A PENTOFURANSOYL MOIETY, PREFERABLY ONE WHOSE 2''-OXYGEN IS TRANS TO THE TRIAZOLE AGLYCON, E.G., XYLOFURANOSYL, RIBOFURANOSYL, R''-OMETHYLRIBOFURANOSYL, ETC., THE TRIAZOLE AGLYCON BEING 3SUBSTITUTED WITH CYANO, METHYLCARBOXYLATE, CARBOXAMIDOXIME, CARBOXYAMIDO-, THIOCARBOXYAMIDO, OR CARBOXAMIDINE. PREPARATION OF THESE NUCLEOSIDES IS BY SILYLATION OF THE SUBSTITUTED TRIAZOLE FOLLOWED BY GLYCOSYLATION WITH THE APPROPRIATE BLOCKED GLYCOSYL HALIDE. ALTERNATIVELY, ACIDCATALYZED FUSION OF THE REQUISITE 1,2,4-TRIZOLE WITH AN O-ACYLATED PENTOFURANOSE YIELDS THE NUCLEOSIDES.
Inventors
- 👤 J Witkowski
- 👤 R Robins
Bibliographic Details
Claims Analysis
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