DERIVATIVES OF PYRROLIDINE, METHOD OF THEIR SYNTHESIS (VARIANTS), PHARMACEUTICAL COMPOSITION, METHOD OF SEPARATION OF ENANTIOMERS AND CHIRAL PHASE FOR SEPARATION OF ENANTIOMERS Russian patent published in 1998 - IPC

FIELD: invention relates to derivatives of pyrrolidine of the formula (I) where R means methylene-, ethylene-radical, groups >SO₂,>SO₂ or sulfur atom; R₁ means pyridinyl, furyl, thienyl that can be substituted, if necessary, with one or some alkyl groups or it means naphthyl, indolyl or phenyl substituted if necessary with one or some substituents taken from halogen atoms, alkyl-, alkoxy-, hydroxy- and dialkylamino-group; R₁ means hydrogen atom and R₅ means phenyl; or R means group >CHR₆; R₁ and R₅ mean hydrogen atom; R₂ means alkoxycarbonyl, cycloalkyl-alkoxy-carbonyl- and others; R₃ means indolyl- or phenylamino-radical phenyl nucleus of that is substituted with one or some substituents taken from the order containing halogen atom, alkyl-, alkoxy-, alkylthio-group and others; R₄ means hydrogen atom and alkyl-radical; R₆ means phenyl-radical in the form of racemic mixture or enantiomers and their salts also. Compounds of the general formula (I) are synthesized by interaction of an active derivative of carbamic acid synthesized by action of N,N-diimidazolecarbonyl on derivative of the general formula (II) with aniline, or by interaction of compound of the general formula (II) with phenylisocyanate, or by interaction of compound of the general formula (IV) with acid HOOC-CH-(R₄)-NH-CO-R₃ or with reactive derivative of this acid. Method of separation of enantiomers of compounds of the formula (I) involves chromatography with chiral phase. Invention relates to also pharmaceutical composition showing activity to cholecystokinin and gastrin receptors that has an active component and pharmaceutical additions and compound of the formula (I) as an active component taken at effective amount. EFFECT: improved method of synthesis. 12 cl, 1 tbl, 120 ex