| 摘要 |
FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention related to derivatives of pyridone of the formula (I') <EMI ID=0.319 HE=54 WI=36 TI=CHI> where R<SB>1</SB> is C<SB>1</SB>-C<SB>4</SB>--alkyl; R<SB>2</SB> - hydrogen; R<SB>3</SB> is SC<SB>6</SB>H<SB>5</SB>,; R<SB>4</SB> is CH<SB>2</SB>OR<SB>13</SB> where R<SB>13</SB> - hydrogen, benzyl; <EMI ID=0.320 HE=3 WI=3 TI=CHI> - tetrazolyl. Method of synthesis of compounds of the formula (I') involves interaction of compound of the formula (II') : AO-CH=C(R<SB>3</SB>)-C(O)R<SB>4</SB> where R<SB>3</SB> and R<SB>4</SB> have values indicated above with compound of the formula (III'): R<SB>1</SB>-CH=C(R<SB>2</SB>)-O-alk where R<SB>1</SB> and R<SB>2</SB> have values indicated above, and alk - alkyl containing 5 carbon atoms, not more. Synthesized compound of the formula (IV') <EMI ID=0.321 HE=24 WI=45 TI=CHI> is saponificated to compound of the formula (V') <EMI ID=0.322 HE=24 WI=42 TI=CHI> and oxidized and formed compound of the formula (VI') <EMI ID=0.323 HE=24 WI=48 TI=CHI> is subjected for reaction of alkylhydroxy-group elimination to compound of the formula (VII') <EMI ID=0.324 HE=21 WI=42 TI=CHI> and the latter is subjected for interaction with compound of the formula (VIII') <EMI ID=0.325 HE=15 WI=66 TI=CHI>. Invention proposes also a pharmaceutical composition showing antagonistic activity with respect to receptors of angiotensin-II and containing compound of the formula (I') as an active component at effective dose. These compounds can be used in medicine. EFFECT: improved method of synthesis, enhanced pharmacological activity of compounds. 4 cl, 1 tbl, 4 ex |
