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Updated: Aug 15, 2026

Preparation of Contiguous Bisaziridines for Regioselective Ring-Opening Reactions
Published on: July 28, 2022
Solid-phase, multicomponent reactions of methyleneaziridines: synthesis of 1,3-disubstituted propanones
Jean-François Margathe1, Michael Shipman, Stephen C Smith
1Department of Chemistry, University of Warwick, Coventry, UK.
Abstract:
[reaction: see text] Polymer-supported methyleneaziridines undergo ring opening by Grignard reagents under copper catalysis to yield metalloenamines which are alkylated in situ to yield ketimines. Filtration and washing of these Merrifield resin-bound intermediates prior to hydrolysis provides the corresponding 1,3-disubstituted propanones in a high state of purity without recourse to column chromatography.
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