Asymmetric Synthesis of Trisubstituted Aziridines via Aza-Darzens Reaction of Chiral Sulfinimines

作者:Moragas Toni*; Churcher Ian; Lewis William; Stockman Robert A
来源:Organic Letters, 2014, 16(24): 6290-6293.
DOI:10.1021/ol502967x

摘要

The aza-Darzens reaction of substituted 2-bromoesters with chiral tert-butane- and mesitylsulfinimines provides a rapid access to a range of highly substituted aziridines in good yields and excellent levels of stereoselectivity. The synthetic potential of this protocol is further enhanced by the successful removal of the sulfinyl motif, yielding simple access to chiral NH aziridines in just three steps from commercial aldehyde precursors.

  • 出版日期2014-12-19