Scalable synthesis of N-acylaziridines from N-tosylaziridines

J Org Chem. 2013 Sep 6;78(17):8865-71. doi: 10.1021/jo401267j. Epub 2013 Aug 27.

Abstract

N-Acylaziridines are important starting materials for the synthesis of chiral amine derivatives. The traditional methods for producing these activated aziridines have significant drawbacks. The gram scale synthesis of N-acylaziridines by deprotection of N-tosylaziridines and reprotection with N-hydroxysuccinimide derivatives is described. Mono- and disubstituted aziridines perform well, with complete retention of stereochemical purity. The consistently moderate yields are linked to the N-tosylaziridine deprotection step, while acylation with N-hydroxysuccinimide derivatives is highly efficient.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Aziridines / chemical synthesis*
  • Aziridines / chemistry*
  • Molecular Structure
  • Tosyl Compounds / chemistry*

Substances

  • Aziridines
  • Tosyl Compounds