Direct C(sp³)–H Polyfluoroarylation: Access to Polyfluoroaryl Amino Acids via Rh-Catalyzed Selective C–F Bond Cleavage

Abstract

A catalytic selective C–F bond alkylation method for polyfluoroarene with glycinates and derivatives in the presence of a DavePhos-ligated Rh catalyst was developed. This method avoids the preactivation of alkylating reagents and provides an efficient and straightforward route to synthesize a series of polyfluoroaryl amino acids via C(sp3)–H functionalization. This reaction proceeds under mild conditions and exhibits high reactivity and excellent chemoselectivities. Meanwhile, the synthetic potential of this method was demonstrated by gram-scale synthesis, and further transformations proved the application value of the products as well.