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.