As originally reported by Logothetis, alkenyl azides cyclize smoothly on warming, leading, depending on substitution, to cyclic imines or bicyclic aziridines. These intermediates can then be carried on to other products. This review summarizes the many ways the Logothetis reaction has been employed in target-directed synthesis.

The assembly of cyclic amines is fundamental to medicinal chemistry. While intramolecular azide–alkyne cycloaddition is widely practiced, intramolecular azide–alkene cycloaddition is much less used, even though it has been known since 1965. This review is an overview of the applications of intramolecular azide–alkene cycloaddition in target-directed synthesis since that time.