One‐Pot Synthesis of Chiral Aziridines by a Domino Reaction by Using Desulfonylative Formation on the N‐Tosyl Imine of Chloroacetaldehyde with an Asymmetric Mannich Reaction as a Key Step

Aziridines with ease: A one-pot synthesis of chiral aziridine derivatives with excellent diastereo- and enantioselectivities was developed through uninterrupted sequential reactions, including desulfonylative formation of the N-Ts imine derived from chloroacetaldehyde, a diarylprolinol silyl ether mediated asymmetric Mannich reaction, reduction, and aziridine formation (see scheme; Ts=tosyl).