Asymmetric Synthesis of Heterocyclic Chloroamines and Aziridines by Enantioselective Protonation of Catalytically Generated Enamines**

Liam A. McLean, Matthew W. Ashford, James W. B. Fyfe, Alexandra M. Z. Slawin, Andrew G. Leach, Allan J. B. Watson

Research output: Contribution to journalArticlepeer-review

Abstract

We report a method for the synthesis of chiral vicinal chloroamines via asymmetric protonation of catalytically generated prochiral chloroenamines using chiral Brønsted acids. The process is highly enantioselective, with the origin of asymmetry and catalyst substituent effects elucidated by DFT calculations. We show the utility of the method as an approach to the synthesis of a broad range of heterocycle-substituted aziridines by treatment of the chloroamines with base in a one-pot process, as well as the utility of the process to allow access to vicinal diamines.

Original languageEnglish
Article numbere202200060
JournalChemistry – A European Journal
Volume28
Issue number16
DOIs
Publication statusPublished - 16 Mar 2022

Keywords

  • Brønsted acid
  • asymmetric catalysis
  • aziridine
  • chloroamine
  • heterocycles

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