Flexible Construction of Functionalized-Pyrroles under Palladium or Copper Catalysis in the Presence of BF₃ ⋅ Et₂O

We have developed a flexible approach enabling the access to highly functionalized pyrroles under palladium or copper catalysis in the presence of BF₃ ⋅ Et₂O. This catalytic methodology utilizes commercially available amines as reaction partners, and features ample scope, scalable and friendly operations with the generation of only water as byproduct. The generality of this protocol is demonstrated by the successful preparation of a range of di-, tri-, tetra- and pentasubstituted pyrroles. This methodology is amenable for the synthesis and derivatization of bioactive compounds. (Figure presented.).