DERIVATIVES OF AMINO(THIO)ESTERS, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF ITS PREPARING Russian patent published in 2000 - IPC

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes the novel derivatives of amino(thio)esters of the formula (I) where X means oxygen, sulfur atom and if R⁰ and R¹ in common are not alkylene chain with 1-3 carbon atoms then CH₂; Z means being n¹ = 0, 1, 2 or 3; n² = 0 or 1; n³ = 0, 1, 2 or 3 at condition that n¹+n²+n³ <4; R⁰ means hydrogen atom or A; R¹ means hydrogen atom, A, OA, phenoxy-group, Ph, OH, F, Cl, Br, CN, CF₃, COOH, COOA, acyloxy-group with 1-4 carbon atoms, carboxamido-group; or R⁰ and R¹ in common are alkylene chain with 1-3 carbon atoms or alkylene chain with 2-3 carbon atoms; R² means hydrogen atom, A, Ac or -CH₂-R⁴; R³ means CH₂-R⁴ or CHA-R⁴ means Ph, 2-, 3- or 4-pyridyl that can be unsubstituted or monosubstituted with R⁴, unsubstituted thiophene or mono- or disubstituted thiophene with A, OA, OH, F, Cl, Br or other thienyl-group; R⁵ means phenyl group that can be unsubstituted or mono-, di-, tri-, tetra- or penta-substituted with F, R⁵, partially or totally fluorinated A, A and/or OA; CF₃ each means independently and/or R⁶, R⁷, R⁸, R⁹ and R¹ in common mean alkylene chain with 3-4 carbon atoms; A means alkyl with 1-6 carbon atoms; Ph means unsubstituted phenyl or phenyl substituted with R⁶, 2-, 3- or 4-pyridyl or phenoxyl-group. Invention relates to physiologically acceptable salts of these derivatives. New compounds effect on central nervous system, especially, as agonists and antagonists of serotonine. They can be used as active components of tranquilizers, antidepressants, neuroleptics and/or hypotensive agents. Invention describes also method of synthesis of compounds of the formula (I) R⁵, pharmaceutical composition based on said and method of composition preparing. EFFECT: new compounds indicated above, valuable pharmacological properties. 9 cl, 1 tbl, 28 ex