DERIVATIVES OF PIPERAZINE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, INTERMEDIATE COMPOUND Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes derivatives of piperazine of the general formula (I) where A means alkylene chain comprising from 2 to 4 carbon atoms optionally substituted with lower alkyl; Z means oxygen or sulfur atom; R means hydrogen atom or lower alkyl; R¹ means unsubstituted phenyl or phenyl mono- or disubstituted with lower alkyl, halide, hydroxy- or lower alkoxy-group; unsubstituted naphthyl of naphthyl substituted with lower alkoxy-group; tetrahydro-naphthyl, isoquinolinyl, indolyl, bicyclic radical of the formula a) or b) ; R² means monocyclic aromatic heterocyclic 6-membered ring comprising one N atom as heteroatom or it means bicyclic aromatic heterocyclic ring system comprising one such 6- membered monocyclic aromatic heterocyclic ring condensed with benzene ring under condition that indicated bicyclic heterocyclic radical is joined with nitrogen of amine of the formula (I) through carbon atom of heterocyclic ring, or R² means thiazolyl; and R³ means lower alkyl, lower cycloalkyl, lower cycloalkenyl, phenyl, cyanophenyl or group of the formula -NR⁴R⁵ where R⁴ means hydrogen atom and R⁵ means lower cycloalkyl, adamantyl or R⁴ and R⁵ in common with nitrogen atom to which they both are joined form piperidino-radical. Invention relates also to method of their synthesis, pharmaceutical composition and intermediate compound, namely 1-(2-methoxyphenyl)-4-[2-(2- pyridinylamino)ethyl] piperazine. New compounds show favorable action on central nervous system by means their ability to bind with 5-HT-receptors. EFFECT: improved method of synthesis, valuable medicinal properties. 10 cl, 71 ex