Highly efficient synthesis of indoline via palladium catalyzed C–H amination of C(sp2)–H bond using tert-butyl peroxybenzoate as an oxidant

A practicable and efficient C–H activation approach for the synthesis of indoline using palladium as the catalyst and tert-butyl peroxybenzoate as the oxidant was firstly reported. A broad range of phenethylamine derivatives with diverse functional groups were well tolerated. Moreover, late-stage diversification of the indoline could proceed successfully and corresponding bioactive molecules were achieved in good yields.