Rh(II)‐catalyzed Intermolecular Benzylic C(sp³)−H Alkylation of Methyl‐substituted Arenes by N‐Aryl‐α‐diazo‐β‐amidoesters

Abstract

Herein, a general approach to intermolecular benzylic C(sp3)−H alkylation of methyl‐substituted arenes is reported using metal carbenes derived from N‐aryl‐α‐diazo‐β‐amidoesters and dirhodium catalysts. Alkylated products were formed in up to 81 % yield with demonstrated functional group tolerance, outpacing previous literature. The unique amide‐ester scaffolding can be exploited through various derivatizations for broad synthetic utility and provides a starting point for the development of selectivity rules and reactivity profiles for these intermolecular C(sp3)−H functionalizations.