FIELD: organic chemistry and technology. SUBSTANCE: products: derivatives of pyridone biphenyl of the formula (I) and their salts where R1 is COOH, C1-C8--alkoxycarbonyl; R2 is C1-C8--alkyl, group -CH2-O-R5 where R5 is C1-C10--alkyl; R3 is hydrogen; R4 is hydrogen, halogen, C1-C6--alkyl, hydroxy-group, C1-C8--alkoxy-group, CF3, CF3O. Reagent 1: compound of the formula (II) where R1 and R2 have above indicated values. Reagent 2: compound of the formula (III) where R3 and R4 have above indicated values; R6 is triphenylmethyltetrazolyl; E is chlorine or bromine. Reaction conditions: in medium of inert solvent, in the presence of base and catalyst if necessary. Compounds of the formula (I) show specific antagonistic effect with respect to angiotensin-II, they inhibit vasoconstrictive and aldosterone secretion stimulating effects of angiotensin-II and proliferation of smooth muscle cells. Synthesized compounds are used in medicine for treatment of patients with hypertension and atherosclerosis. EFFECT: improved method of synthesis, enhanced effectiveness of compounds.
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Authors
Dates
1998-09-20—Published
1993-10-22—Filed