METHOD FOR PRODUCTION OF (2R)-METHYL-4,4,4-TRIFLUOROBUTYL AMINE OR ITS ACID ADDITIVE SALT, 4,4,4-TRIFLUORO-2-METHYL-N(3S)-1-PHENYLETHYLBUTYRAMIDE AND (2R)-METHYL-4,4,4-TRIFLUOROBUTYL(1S)-PHENYLETHYL AMINE OR ITS ACID ADDITIVE SALT AND METHOD FOR PRODUCTION OF (R)-4-5-(N4,4,4-TRIFLUORO-2-METHYLBUTYL-CARBAMOYL)-1-METHYLINDOL- 3-YL-METHYL-3-METHOXY-N-ORTHOTOLYLSULFONYL BENZAMIDE

摘要

FIELD: organic chemistry. SUBSTANCE: -C₁-C₆-alkylbenzyl amine is acylated by 2-methyl-4,4,4-trifluorobutyric acid or by its reactive derivative to prepare racemate of appropriate butyramide. Then (R)-diastereomer butyramide is separated of (S)-diastereomer butyramide. Thus separated (R)-diastereomer is then reduced to appropriate amine. Thus obtained amine is affected by hydrogenolysis to isolate desired product as a base or its acid additive salt. Product of said reaction is acylated by carboxylic acid having formula I or by its reactive derivative to prepare (R)-4-[5-(N[4,4,4-trifluoro-2-methylbutyl] -carbamoyl)-1-methylindol- 3-yl-methyl] -3-methoxy-N-orthotolylsulfonyl benzamide. Structure of compound having formula I is given in specification. EFFECT: improves efficiency of method, improves quality of desired product. 9 cl