Catalytic Enantioselective Desymmetrization of meso-N-Acylaziridines with TMSCN

摘要

Chiral beta-amino acids are important building blocks for natural products and Pharmaceuticals.Among them,chiral cyclic beta-amino acids are currently of great interest due to the recent finding that peptides composed of these amino acids can act as foldamers with a well-defined secondary structure.Despite the emerging importance,there are few enantioselective synthetic methods that produce chiral cyclic beta-amino acids.Specifically,there is no method available using an artificial enantioselective catalyst to access these compounds.Here,we describe the first such method based on the catalytic enantioselective desymmetrization of meso-aziridines by cyanide.