Synthesis and Characterization of β-Trifluoromethyl-Substituted Pyrrolidines

A practical synthetic approach to the construction of a library of three isomeric/homologous beta-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.