Site-Selective C8-Alkylation of Quinolines with Cyclopropanols: Merging C-H/C-C Bond Activation.

Abstract

The site-selective C8-alkylation of quinolines has been accomplished using cyclopropyl alcohols as the alkylating agents and N-oxide as a weak chelating group in the presence of Co(III) catalysis via merging C-H/C-C bond activation. The use of cyclopropanol as the alkyl source, Co catalysis, substrate scope, HRMS analysis of the reaction intermediate, and late-stage mutation of drug molecules/natural products are the important practical features.