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2000
Volume 22, Issue 6
  • ISSN: 1570-1794
  • E-ISSN: 1875-6271

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.

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Base Mediated 7-exo-dig Intramolecular Cyclization of Betti-propargyl Precursors: An Efficient Approach to 1,4-oxazepine Derivatives
Curr. Org. Synth. 22, 747 (2025); https://doi.org/10.2174/0115701794353226241209175136
/content/journals/cos/10.2174/0115701794353226241209175136
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  • Article Type:     Research Article
Keyword(s): 1,4-oxazepine; 7-exo-dig cyclization; betti reaction; biological activity; multi-component reactions; propargyl bromide

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