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Base Mediated 7-Exo-Dig Intramolecular Cyclization of Betti-Propargyl Precursors: An Efficient Approach to 1,4-Oxazepine Derivatives Publisher Pubmed



Yazzaf R ; Asadi M ; Mahdavic M
Authors

Source: Current Organic Synthesis Published:2025


Abstract

Introduction: 1,4-oxazepine is a significant structural motif found in several bioactive molecules used in the treatment of diseases such as psychotic disorders. Methods: Therefore, developing novel methodologies for its preparation is of great interest to medicinal chemists. Results: These seven-membered heterocycles are generated through the intramolecular cyclization of Betti bases, which are propargylated using propargyl bromide as the source of the triple bond in the presence of a base. Conclusion: This efficient and straightforward protocol proceeds under mild, metal-free conditions and has been shown to be applicable to a broad range of aldehydes and 2-aminopyridines. © 2025 Elsevier B.V., All rights reserved.