Methods for the Synthesis of Substituted Azetines
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Updated: Feb 21, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Andreas N Baumann1, Michael Eisold1, Arif Music1
1Department of Chemistry and Pharmacy, Ludwig-Maximilians-University , Butenandtstraße 5-13, 81377 Munich, Germany.
Abstract:
Spurred on by the recent emerging interest from the chemical community for unsaturated four-membered heterocycles, an unprecedented approach to nitrogen-containing four-membered rings has been designed. 3,4-Disubstituted 2-azetines were synthesized from commercially available substrates, allowing for a straightforward access to a new library of chiral functionalized azetidines and amino alcohols. This original approach was applied to efficiently prepare functionalized azobenzenes, an emerging class of molecules with a large potential in photopharmacology.
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