BENZENESULFONAMIDE DERIVATIVES OF PYRIMIDINE OR THEIR SALTS, PHARMACEUTICAL COMPOSITION FOR TREATMENT OF DISEASES ASSOCIATED WITH ENDOTHELIN ACTIVITY Russian patent published in 1997 - IPC

FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: product: benzenesulfonamide derivatives of pyrimidine of the formula (I) where: R₁ - hydrogen, lower alkyl, lower alkylhydroxy-group; R₂ - hydrogen; R₃ - hydrogen, halogen, lower alkyl, trifluoromethyl, lower alkoxy-group; R₂ and R₃ together form methylenedihydroxy-group; R₄ - hydrogen, lower alkyl, trifluoromethyl, phenyl, furyl, pyrimidinyl, pyridyl, pyridyl-N-oxide; R₅ - hydrogen, lower alkanoyl; R₆-R₉ - hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio-group or methylsulfinyl; R₇ together with R₆ or R₈ - butadienyl or -OCH₂O-; Z - -O-, vinyline; X and Y - -O- and n = 2, 3 or 4, or their salts. Reagent 1: compound of the formula (II) . Reagent 2: MX(CH₂)_nYR₅; M - alkaline metal or reagent 1 of the formula (III) (R₁R₂R₃)C₆H-CH₂P^⊕(Q)₃A^-; Q=aryl , or reagent 2 of the formula (IV) where: Q - aryl, A - anion followed by hydrogenation or their salts. Pharmaceutical composition is used for treatment of diseases associated with endothelin activity and has benzenesulfamide derivatives of pyrimidine of the formula (I) taken at doses 0.1-100 mg/kg and pharmaceutically acceptable carrier. EFFECT: improved method of synthesis. 2 tbl