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<p>The azetidine group is frequently encountered within
contemporary medicinal chemistry where it is viewed as a privileged structure.
However, the introduction of an azetidine can be synthetically challenging. Herein,
a straight-forward one step synthesis of azetidine-3-amines, starting from a bench
stable, commercial material is presented. The reaction tolerates functional
groups commonly encountered in biological-, medicinal- and agro-chemistry, and
proceeds in moderate-to-high yield with secondary amines, and moderate-to-low
yield with primary amines. The methodology compares favorably to recent alternative
procedures and can be utilized in “any-stage” functionalization, including late-stage
azetidinylation of approved drugs and other compounds with pharmacological
activity.</p>
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A Single-Step Synthesis of Azetidine-3-Amines