PIPERIDINYL-SUBSTITUTED METHANOANTHRACENES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, A PHARMACEUTICAL COMPOSITION BASED ON SAID AND METHODS OF THEIR SYNTHESIS Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to piperidinyl-substituted methanoanthracenes of the formula (I) where X and Y mean hydrogen atom; R₁ means pyridyl substituted with chiral (1-4C)-alkylsulfinyl-group and their pharmaceutically acceptable salts. Invention relates to also a pharmaceutical composition showing antagonistic activity with respect to Д1/Д2-dopamine and serotonine receptors and containing a compound of the formula (I) as an active component taken at effective dose. Invention relates to also a method of synthesis of compounds of the formula (I) by chiral oxidation of a compound of the formula (I) where X and Y - hydrogen atom; R₁ - pyridyl substituted with (C₁-C₄)-alkyl-S-group. For enantioselective oxidation a group (C₁-C₄)-alkyl-S is oxidized to chiral sulfoxide of the formula (C₁-C₄)-alkyl-SO. Obtained compound (I) is isolated or converted to a pharmaceutically acceptable salt which can be used as dopamine antagonists and as an antipsychotic agent for patients treatment. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 10 cl, 5 dwg, 4 ex