Rh(iii)-catalyzed enantioselective C–H arylation: atroposelective synthesis of 2-pyridones from diazo compounds

Abstract

Axially chiral scaffolds are privileged motifs in natural products, bioactive agents, and asymmetric catalysis. Here, we present an enantioselective C–H arylation of 2-pyridones at the C6 position with diazo compounds, catalyzed by a chiral Rh(III) complex. This strategy enables direct, efficient, and modular construction of C–C axially chiral 2-pyridones with high yields and outstanding enantioselectivity (up to 99% yield, 99% ee). The method features a broad substrate scope, operational simplicity, and scalability, offering a versatile and practical route to diverse useful atropisomeric architectures.