QUINUCLIDINE ESTERS, INTERMEDIATE COMPOUNDS FOR ITS SYNTHESIS, PHARMACEUTICAL COMPOSITION AND A METHOD OF TREATMENT Russian patent published in 1998 - IPC

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to derivatives of 3-quinuclidyl esters of the formula (I) or its pharmaceutically acceptable acid-additive salts where X - phenyl; Y - group where A and B = 0, 1 or 2 independently; Z = 0, 1 or 2; R¹ and R²- - independently hydrogen atom, -alkyl; R₃ - -alkyl or phenyl. Compounds show antagonistic activity with respect to muscarinic receptors. Invention relates to also pharmaceutical composition exhibiting antimuscarinic bronchodilating effect that has above described compound or its salt at effective amount in mixture with pharmaceutically acceptable carrier or vehicle and to method of bronchodilation that involves administration of the above described compound at effective amount. Invention proposes also intermediate ester derivatives of quinuclidine of the formula (II) where X - phenyl; Y - group R₁ , R₂ where A, B, R₃ and have values indicated above. Method of synthesis of compounds of the formula (I) involves interaction of compound of the formula (II) with strong base followed by interaction of the obtained carbanion with formaldehyde and producing compound of the formula (I) where Z = 0. If necessary, compound of the formula (I) where Z = 0 is oxidized to compound of the formula (I) where Z = 1 or 2. If necessary, compound of the formula (I) can be converted to its pharmaceutically acceptable salt. EFFECT: improved method of synthesis, enhanced effectiveness of compounds synthesized. 17 cl, 19 proc, 30 ex, 6 tbl