Atroposelective Dynamic Kinetic Resolution via In Situ Hemiaminals Catalyzed by N-Heterocyclic Carbene

Axially chiral amino acids and its derivatives are vital building blocks of bioactive molecules, artificial peptides, and asymmetric catalysts. Herein, we report an unprecedented carbene-catalyzed atroposelective dynamic kinetic resolution to access axially chiral amino esters via in situ hemiaminals. This protocol features a broad substrate scope and good functional group tolerance and allows the rapid assembly of axially chiral amino esters in good to high yields with high enantioselectivities.

Automated summary

The novel method described in this report allows for the atroposelective generation of axially chiral amino esters using hemiaminals formed in situ, with a wide substrate scope, good functional group tolerance, and rapid assembly of axially chiral amino esters with high enantioselectivities in good to high yields.