XANTHINE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD OF SYNTHESIS OF XANTHINE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, PHARMACEUTICAL COMPOSITION

摘要

FIELD: organic chemistry, purines. SUBSTANCE: derivatives of xanthine containing direct or branched C₃-C₆-alkyl, alkenyl or alkynyl at N1-atom of pyrimidine ring; N2-atom can be substituted with phenyl containing substituents at meta- and ortho-positions that can be similar or different (hydrogen, halogen, methyl-. methoxy-, nitro- or trifluoromethyl-group), or substituents form together methylenedioxy- or ethylenedioxi-group at condition that both these radicals are not hydrogen simultaneously, or their pharmaceutically acceptable salts. Derivatives were synthesized by treatment of the corresponding 6-aminouracil with sodium nitrite and formic acid in formamide excess with addition of sodium dithionite to reduce the synthesized 6-amino-5-nitrosouracil to the corresponding amine. The latter is condensed with formamide and xanthine derivatives were obtained being 6-amino-5-nitroso-derivatives and 5,6-diamine were formed in situ. Pharmaceutical composition has pharmaceutically acceptable carrier or diluting agent and above indicated xanthine derivative as an active substance taken at effective amount. Synthesized compounds were used in medicine to eliminate states when phosphodiesterase type IV is inhibited significantly. EFFECT: improved method of synthesis, enhanced effectiveness. 8 cl, 2 tbl