Gerus I. Synthesis of new fluorine-containing bioactive compounds based on β- alkoxyvinyl polyfluoroalkyl ketones

Synthesis of fluorinated analogues of bioactive compounds: amino and hydroxy acids and heterocycles. Development of new methods for the synthesis of polyfluoroalkyl-containing α,β-unsaturated ketones and obtaining new analogues of natural bioactive compounds and the study of physicochemical and biological properties of synthesized substances.Chemical synthesis, high performance liquid chromatography, TLC, IR spectroscopy, NMR spectrometry. New fluorinated reagents for the synthesis of polyfluoroalkyl-containing: ornithine, GABA, enaminones and various heterocyclic compounds are proposed. A new electrocyclic reaction for the conversion of fluoroalkyl-containing α,β-unsaturated ketones with a dioxolane moiety into mono- and difluoromethylene-containing cyclopentenones was found and investigated. An effective reagent for the protection of the amino group of amino acids in peptide synthesis has been proposed and developed. β-Polyfluoroalkyl-containing GABA analogues were obtained and a comparative analysis of their effect on the accumulation of [3H] GABA by synaptosomes of mice was performed with GABA transporter inhibitor - Pregabalin: the efficacy of β-CF3-β-OH-GABA and β-CНF2CF2-GABA is higher than that of Pregabalin. Scope - bioorganic chemistry.