FIELD: chemistry.
SUBSTANCE: invention relates to an improved method of producing substituted 3-arylbutylamine compounds of general formula I, meant for use as pharmaceutical active substances in medicinal agents and primarily suitable for pain killing. The proposed method of producing compounds of formula I 
in which R1 is H or branched or unbranched, saturated unsubstituted C1-C3alkyl, R2 and R3 independently represent H or branched or unbranched, saturated unsubstituted C1-C4alkyl, R4 is H or branched or unbranched, saturated unsubstituted C1-C3alkyl, R7 and R8 independently represent H or branched or unbranched, saturated unsubstituted C1-C4alkyl, R9-R13 independently represent H, OH, OR14, R14 is C1-C6alkyl, CONH-C6H5-(C1-C3alkyl), where alkyl groups in the R14 residue can be branched or unbranched, saturated unsubstituted, in each case in form of one of its pure stereoisomers, primarily enantiomers or diastereomers, its racemates or in form of a mixture of stereoisomers, primarily enantiomers of diastereomers, in any ratio in the mixture or in each case in form of a physiologically compatible salt, involves carrying out stage a) elimination of 1-amino-3-arylbutan-3-ol of general formula 
in which R1, R2, R3, R4, R7, R8, R9, R10, R11, R12 and R13 assume values given above, in each case possibly in form of one of its pure stereoisomers, primarily enantiomers or diastereomers, its racemates or in form of a mixture of stereoisomers, primarily enantiomers or diastereomers in any ratio in the mixture or in each case in form of a physiologically compatible salt, under the effect of the corresponding acid to obtain a substituted 3-arylbut-3-enylamine compound of general formula III, and then at second step b) the formed substituted 3-arylbut-3-enylamine compound of general formula III is hydrogenated in the presence of a palladium catalyst and hydrogen to obtain the corresponding substituted 3-arylbutylamine compound of general formula I.
EFFECT: method simplifies the process due to possibility of carrying out the process in a single apparatus without extraction of intermediate products with provision for enantiomeric purity during conversion of stereochemically pure compounds.
90 cl, 19 ex
