A highly efficient method for the construction of cyclopropane-containing dihydroindole derivatives from indolemethylenecyclopropanes with DIAD and DEAD

A highly efficient method for the construction of cyclopropane-containing dihydroindole derivatives from indolemethylenecyclopropanes with DIAD and DEAD has been disclosed. The transformation could occur under catalyst-free conditions at ambient temperature to afford dihyroindole derivatives in good yields. It has been proved that the strained moiety of methylenecyclopropane in the substrate of indolemethylenecyclopropane is critical and DFT calculations reveal that the reaction proceeds through a two-step pathway.