FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: product: derivatives of 9-deazaguanine of the formula (I): where: CH2-Ar: where: R1 - hydrogen, halogen, / CI- C/ /-alkyl, / CI-C3 /-alkoxy, benzylhydroxy, hydroxy, trifluoromethyl; R2 - hydrogen, halogen, / CI- C3 /-alkoxy, benzylhydroxy, hydroxy, trifluoromethyl under condition: if R2 - hydrogen or / CI- C3 /-alkyl then R1 - trifluoromethyl, or R1 - hydrogen, / CI- C3/-alkyl; if R2 - trifluoromethyl or CH2-Ar - where x - sulfur, oxygen then linkage with thiophene or furan ring is located at 2 or 3 position, or their tautomers. Compounds of the formula (I) were synthesized by interaction of reagent 1 of the formula: where: R3 and R5 - lower alkyl; R4 - carbocyclic aryl, and reagent 2: anhydrous ammonia followed by cyclization and if necessary the protective groups splitting off. Invention relates to also the pharmaceutical composition containing 9-deazaguanine derivative of the formula (I) or its tautomer as an active component taken at amount 0.1-75%, preferably at amount 1-50%, and pharmaceutically acceptable carrier that shows capability to inhibit mammal purine nucleoside phosphorylase activity. EFFECT: improved method of synthesis. 5 tbl
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Authors
Dates
1997-10-20—Published
1991-08-26—Filed