A facile synthesis toward C2-perfluoroalkylated free (NH)-indoles with excellent regioselectivity.

A simple, efficient and mild strategy has been developed for the synthesis of C2-perfluoroalkylated (NH)-indoles from indoles and perfluoroalkyl iodides, with DIPEA serving as the sole base. This protocol furnishes structurally diverse perfluoroalkylated indoles in good yields, features broad substrate scope and excellent functional group tolerance, and is operationally facile, thus showing great potential for synthetic applications.