Rapid Microwave‐Assisted, Solvent‐Free Approach to Functionalization of 8‐Methylquinolines via Rh‐Catalyzed C(sp³)‐H Activation

Abstract

A microwave‐assisted method for the synthesis of 8‐methylquinoline derivatives via Rh‐catalyzed C(sp3)‐H activation under solvent‐free condition is reported. In comparison with traditional method, this reaction proceeded more efficiently with excellent yield, a broad range substrate scope and good functional group tolerance.

Cp*Rh(III)-Catalyzed Regioselective C(sp3)–H Methylation of 8-Methylquinolines with Organoborons

“…Among various transition metal catalysts, a rhodium­(III) catalyst has been well explored for C­(sp 2 )–H bond functionalization reactions due to its high efficiency and selectivity, whereas the functionalization of more challenging C­(sp 3 )–H bonds has not been explored much . Recently, Rh­(III)-catalyzed transformation has been reported for the functionalization of 8-methylquinoline through C­(sp 3 )–H bond activation; however, the methylation/alkylation of 8-methylquinolines using a Rh­(III) catalyst has not yet been explored.…”