Noncovalent organocatalytic synthesis of enantioenriched terminal aziridines with a quaternary stereogenic center

Org Lett. 2012 Aug 17;14(16):4078-81. doi: 10.1021/ol3017066. Epub 2012 Aug 2.

Abstract

A high-yielding and enantioselective access to novel N-Boc terminal aziridines, bearing a quaternary stereogenic center, has been developed via an aza-Michael initiated ring-closure (aza-MIRC) reaction of α-acyl acrylates with an N-tosyloxy tert-butyl carbamate catalyzed by a chiral amino thiourea. The feasibility of the aziridine regioselective ring-opening to valuable α,α-disubstituted α-amino acid esters has been demonstrated.