N-CYCLOPROPYLPIPERIDINE-2-CARBOXYLIC ACID 2,6-DIMETHYLANILIDES AND PHARMACEUTICALLY ACCEPTABLE SALTS WITH ACIDS AND A METHOD OF THEIR SYNTHESIS

摘要

FIELD: organic chemistry and technology. SUBSTANCE: invention relates to new N-cyclopropylpiperidine- -2-carboxylic acid 2,6-dimethylanilides of the formula (I) <EMI ID=0.128 HE=24 WI=39 TI=CHI> where R - cyclopropyl or methylcyclopropyl as a racemic mixture or separate enantiomers or their salts. Method of synthesis of compounds of the formula (I) involves an interaction of 2,6-dibromohexanoyl chloride with 2,6-dimethylaniline in an aprotonic solvent in the presence of the second base equivalent at 0-25 C that results to synthesis of 2,6-dibromohexanoic acid 2,6-dimethylanilide followed by its cyclization in the presence of cyclopropyl- or methylcyclopropylamine and two equivalents of a base in an aprotonic solvent at 70-100 C. Synthesized compounds show enhanced antiarrhythmic and local anesthetic properties and can be used in medicine. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 5 cl, 3 dwg, 3 ex