Pd/NHC sequentially catalyzed atroposelective synthesis of planar-chiral macrocycles

Abstract

Planar-chiral macrocycles play a pivotal role in host–guest chemistry and drug discovery. However, compared with the synthesis of other types of chiral compounds, the asymmetric construction of planar-chiral macrocycles still remains a forbidding challenge. Herein, we report a sequential palladium and N-heterocyclic carbene catalysis to build planar-chiral macrocycles. This protocol features broad scope and good functional group tolerance, and allows a rapid assembling of planar-chiral macrocycles with excellent enantioselectivities.