O-SUBSTITUTED DERIVATIVES OF 6-METHYLTRAMADOL, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION Russian patent published in 2006 - IPC C07C217/74 C07D333/32 A61K31/135 A61K31/381 A61P29/00 

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention relates to novel O-substituted derivatives of 6-methyltramadol of the general formula (I) being optionally as their racemates, their pure stereoisomers but primarily as enantiomers or diastereomers, or as mixtures of stereomers being primarily as enantiomers or disatereomers in any their ratio in the mixture as a presented formulation or as their physiologically compatible salts. In the general formula (I) the value R means hydrogen atom (H), (C₁-C₃)-alkyl that can be saturated or unsaturated, branched or a direct, unsubstituted or substituted with -O-(C₁-C₃)-alkyl-group or OH-group, -CH₂-(C₄-C₆)-cycloalkyl, (C₄-C₆)-cycloalkyl or thienyl group. Also, the invention relates to a method for synthesis of compounds of the general formula (I) by interaction of 2-dimethylaminomethyl-6-methylcyclohexanone of the formula (I) with metal-organic compound of the formula (III) wherein Z means Li; R has values given in the formula (I). The synthesized compounds of the formula (I) if necessary are converted to their physiologically compatible salts and/or racemates that are subjected for cleaving. Also, invention relates to a pharmaceutical composition.

EFFECT: improve method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

8 cl, 2 sch, 2 tbl, 30 ex