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,… Click to show full abstract
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.
               
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