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Abstract
1,4-oxazepine is a significant structural motif found in several bio-active molecules used in the treatment of diseases such as psychotic disorders. Therefore, developing novel methodologies for its preparation is of great interest to medicinal chemists. These seven-membered heterocycles are generated through the intramolecular cy-clization of Betti bases, which are propargylated using propargyl bromide as the source of the triple bond in the presence of a base. 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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