Weak Chelation-Assisted C4-Selective Alkylation of Indoles with Cyclopropanols via Sequential C–H/C–C Bond Activation

A Rh-catalyzed weak chelation-guided C4-alkylation of indoles has been accomplished using cyclopropanols as an alkylating agent via the cascade C–H and C–C bond activation. The substrate scope, functional group tolerance, and late-stage mutation of drug molecules are the important practical features.