Recent advances in synthesis of nitrogen-centered chiral compounds

Nitrogen-centered chiral compounds are widely found in natural products and pharmaceuticals, and can serve as multifunctional chiral catalysts, reagents, and ligands in asymmetric synthesis. However, the creation of nitrogen stereocenters remains a significant challenge. This difficulty arises from the low energy barrier for pyramidal inversion of the amine lone pair, which leads to rapid racemization. In recent years, breakthroughs in areas such as dynamic kinetic resolution, chiral ligand control, enzymatic catalysis, and organocatalysis have dramatically enhanced the efficiency of accessing configurationally stable nitrogen-centered chiral compounds. Herein, we present a detailed overview of the research progress in this field over the past five years, organized by the coordination number of the nitrogen stereocenter.