Rhodium‐Catalyzed Selective C−H Alkenylation of Indole at C4 Position

Abstract

The indole motifs play a significant role in the pharmaceutical exploitation and the synthesis of naturel products, and transition metal catalyzed selective CÀ H bond activation of indoles has received extensive attention. However, the functionalization of CÀ H bonds on the benzene core is still a great challenge. By installing a bulky protecting group on the nitrogen and under the assistance of an ester directing group, we realized the Rh-catalyzed alkenylation of indole at C4 position with high efficiency. This catalytic method exhibits satisfactory functional group compatibility and regioselectivity.