The azetidine group is frequently encountered within contemporary medicinal chemistry. However, the introduction of an azetidine can be synthetically challenging. Herein, a straightforward synthesis of azetidine-3-amines, starting from a bench stable, commercial material is presented. The reaction tolerates common functionality and proceeds in moderate-to-high yield with secondary amines, and moderate-to-low yield with primary amines. The methodology compares favorably to alternative procedures and can be utilized in “any-stage” functionalization, including late-stage azetidinylation of approved drugs and other compounds with pharmacological activity.

中文翻译：

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氮杂环丁烷-3-胺的一步合成。

在现代药物化学中经常遇到氮杂环丁烷基团。然而，氮杂环丁烷的引入可能在合成上具有挑战性。本文中，提出了从稳定的市售材料开始的氮杂环丁烷-3-胺的直接合成。该反应具有通用的功能性，仲胺的产率中等至高，伯胺的产率中等至低。该方法优于其他方法，可用于“任何阶段”的功能化，包括批准药物和具有药理活性的其他化合物的后期氮杂环丁烷化。