Ligand-controlled regioselective cascade C-C/C-F cleavage/annulation of gem-DFCPs: a divergent synthesis of pyrroles

Herein, a ligand-controlled regioselective ring-opening/defluorinative annulation of gem-DFCPs with enaminones is reported. In the presence of a palladium catalyst, the reaction enables regiodivergent synthesis of pyrroles with different phosphine ligands. The reaction exhibited broad substrate scope and produced a wide range of pyrroles in moderate to good yields. In addition, the annulation process has been applied in the divergent synthesis of some bioactive skeletons.