Synthesis and characterization of β-trifluoromethyl-substituted pyrrolidines

摘要

A practical synthetic approach to the construction of a library of three isomeric/homologous β-trifluoromethyl-substituted pyrrolidines is disclosed. All products were prepared in multigram quantities from a common precursor. The key synthetic step was a [3+2] cycloaddition reaction. The influence of the trifluoromethyl group on the physicochemical characteristics of the pyrrolidine fragment was studied. Three β-(trifluoromethyl)ated pyrrolidines have been synthesized on multigram scales. The influence of the CF_3 group on the physicochemical properties of the pyrrolidine fragment has been studied.