Advances in Direct Fluoroalkylation of Organic Substrates with Partially Fluorinated Alkyl Motivs

Abstract

Partially fluorinated alkyl groups other than methyl are increasingly playing crucial roles in the development of fluorinated drugs with diverse biological activities, thus creating an innovative chemical space within organofluorine chemistry. For studies of structure–activity relationships, late-stage modification with such groups or substituents into substrates that bear biological activity is essential. This perspective will study catalytic protocols for the direct introduction of partially fluorinated alkyl groups such monofluoroalkylated (−CHFR, –CH₂CH₂F), difluoroalkylated (−CF₂Me, –CH₂CF₂H), trifluoroalkylated (−CHR(CF₃), –CH₂CF₃, –CH₂CH₂CF₃, –CH(Me)CF₃, –C(Me)₂CF₃), and pentafluoropropylated (−CH₂C₂F₅) onto (hetero)aromatic compounds, double bonds, isonitriles, alkyl halides, and N, O, and S atoms.