The ubiquity of strained motifs in drug discovery has recently witnessed a large regain of interest, as such scaffold can be used to modulate the properties of drug candidates. Unsaturated N-containing four-membered heterocycles present unique opportunities to access functionalized azetidines, which play an essential role in pharmacological studies. Even though those unsaturated patterns have been much less reported than the corresponding saturated versions, the consequent impact that those structures could have on molecular design with implementation of strained modules deserves to be summarized. In this review, synthetic accesses to substituted azetes, 1-azetines and 2-azetines are depicted, as well as their involvement in further transformations.

药物发现中普遍使用的应变基序最近引起了人们的广泛关注，因为这种支架可用于调节候选药物的性质。不饱和ñ含四元杂环提出了独特的机会来访问功能氮杂环丁烷，这在药理研究起到了至关重要的作用。即使与相应的饱和版本相比，这些不饱和模式的报道要少得多，但这些结构可能对使用应变模块实现的分子设计产生的影响值得总结。在这篇综述中，描述了对取代的氮杂环丙烷，1-氮杂环丁烷和2-氮杂环丁烷的合成途径，以及它们参与进一步的转化。