3'-(5-R-TETRAZOLE-2-YL)-THYMIDINES SHOWING ANTIVIRAL ACTIVITY AND METHOD OF THEIR SYNTHESIS

FIELD: organic chemistry, chemistry of nucleosides. SUBSTANCE: invention describes new 3'-(5-R-tetrazole-2-yl)-thymidines of the formula (I) where R - hydrogen or lower alkyl exhibiting antiviral activity with respect to human immunodeficiency virus (HIV) and avian myeloblastosis virus (AMV), a...

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Hauptverfasser: IVANOVA N.V, POPLAVSKIJ V.S, PASHKOVA T.A, KHOKHRJAKOVA N.R, MALIN A.A, STUDENTSOV E.P, OSTROVSKIJ V.A, KARAMOV EH.V, GULEVSKIJ S.G
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, chemistry of nucleosides. SUBSTANCE: invention describes new 3'-(5-R-tetrazole-2-yl)-thymidines of the formula (I) where R - hydrogen or lower alkyl exhibiting antiviral activity with respect to human immunodeficiency virus (HIV) and avian myeloblastosis virus (AMV), and a method of synthesis of 3'-(5-R-tetrazole-2-yl)-thymidines. Method involves treatment of 5'-O-protected 2,3'-anhydrothymidine with tetrazole derivative of the general formula (II) where R - as indicated above in the presence of trialkylamine in medium of aprotonic dipolar solvent followed by hydrolytic splitting off a protective 5'-O-benzoyl group and isolation of the end product. Synthesized compounds are used in medicine for treatment of patients and animals with viral infections. EFFECT: new thymidine derivatives indicated above, improved method of synthesis. 2 cl, 3 tbl, 3 exi