TFA‐Prompted/Rh(III)‐Catalysed Chemoselective C3− or C2−H Functionalization of Indoles with Methylenecyclopropanes

Abstract The TFA‐prompted/Rh(III)‐catalysed chemoselective C 3 −H alkylation, C 2 −H dienylation and cyclopropylation of indoles have been realized by virtue of methylenecyclopropanes as the versatile coupling partners. This protocol features broad substrate/functional group compatibility and tunable regio‐/chemoselectivity. Diversified derivatization of the obtained products has been also successfully demonstrated, which further strengthened the potential for the synthetic utility of the developed protocols.