Abstract 

Aziridines, are crucial motifs embedded in numerous natural products.1In the  meanwhile, they are of great value for building block utility in organic synthesis.2 

Figure 1 Aziridine-containing natural products 

Nevertheless, the enantio-enriched N-H aziridine preparation has been scarcely  reported. Based on the continuous investigation of copper hydride in our group3, the  asymmetric reduction of 2H-azirines employing the catalytic amount of copper salt, chiral  ligand, and stoichiometric silane has been studied. The investigation mainly involves the  effect of different reductive silanes, nonracemic ligands, and temperatures. Finally, the  aziridine could be obtained in 92% yield and 94:6 er. 

Reference: 

1. F. M. D. Ismail, D. O. Levitsky, V. M. Dembitsky, Eur. J. Med. Chem. 2009, 44, 3373. 2. Schneider, C. Angew. Chem., Int. Ed. 2009, 48, 2082. 
2. Y. Shi, J. Wang, Q. Yin, X. Zhang, P. Chiu, Org. Lett. 2021, 23, 5658 – 5663.