SELECTIVE CARBOXYL ESTERASE INHIBITORS REPRESENTING ALKYL-2-ARYLHYDRAZINYLIDENE-3-OXO-POLYFLUOROALKYLPROPIONATES, METHODS FOR PRODUCTION AND USE THEREOF Russian patent published in 2016 - IPC C07C251/74 A61K31/215 A61K31/15 A01N33/26 

FIELD: chemistry.

SUBSTANCE: invention relates to alkyl-2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates of general formula where R¹= polyfluoroalkyl: for C=1 F=2-3, for C=2 F=2-5, for C=3 F=2-7; R²=Me, Et; R³=H, Alk, AlkO, NO₂. The alkyl-2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates of general formula I are obtained by reacting equimolar amounts of a mixture which is obtained in advance from equivalents of arylamine and sodium nitrite in an aqueous hydrochloric acid solution, and fluorinated 3-oxoether in the presence of a buffer in a water-organic solvent medium, wherein the process is carried out using a chlorohydrocarbon as the organic solvent in the presence of a tetraalkylammonium halide. The alkyl-2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates of general formula I are used as general selective inhibitors of carboxyl esterase, including as selective inhibitors of human carboxyl esterase, insect carboxyl esterase and rodent plasma carboxyl esterase. The alkyl-2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates of general formula I are used as a pharmacological agent or in a pharmaceutical composition or a pesticide formula, metabolism- and pharmacokinetic-regulating medicinal drugs containing ester or amide groups.

EFFECT: alkyl-2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates as effective and selective carboxyl esterase inhibitors for improving the effectiveness of medicinal drugs and pesticides containing ester and amide groups.

9 cl, 2 tbl, 1 dwg, 6 ex