Convenient Access to Di‐ and Tri­fluoroethylamines for Lead Structure Research

Abstract

Much research effort has been devoted to the synthesis of fluorinated organic compounds in medicinal chemistry programs. For instance, incorporation of fluorine substituents and trifluoromethyl groups has become a widespread lead optimization strategy owing to the often favorable influence of such moieties on affinity and physicochemical properties. However, introduction of fluoroalkyl groups into dedicated positions of pharmacophores is synthetically challenging. In particular, efficient syntheses of di-and trifluoroethylamines are needed as

One-Pot Synthesis of Substituted Trifluoromethylated 2,3-Dihydro-1H-imidazoles

“…Recently, we reported the usage of shelf-stable trifluoroacetaldehyde-derived hemiaminal ether building blocks to efficiently access functionalized di- and trifluoromethylated N -aryl amine derivatives . In the course of these studies, we also observed formation of unprecedented pentasubstituted 2,3-dihydro-1 H -imidazoles, bearing a CF 3 group at C-2 and an additional fluorine substituent at C-4 (Figure ).…”