Azetidines possess a favorable balance between satisfactory stability and strong molecular rigidity, enabling efficient adjustment of pharmacological properties exhibited by molecules containing this moiety. Consequently, azetidine is regarded as a favored framework in the realm of drug discovery.

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[1]Antermite D, Degennaro L, Luisi R. Recent advances in the chemistry of metallated azetidines[J]. Organic & Biomolecular Chemistry, 2017, 15(1): 34-50.

[2]Kirichok A A, Shton I O, Pishel I M, et al. Synthesis of multifunctional spirocyclic azetidines and their application in drug discovery[J]. Chemistry–A European Journal, 2018, 24(21): 5444-5449.

[3] Ye Y, Wang H, Fan R. Stereoselective construction of highly functionalized azetidines via a [2+ 2]-cycloaddition[J]. Organic Letters, 2010, 12(12): 2802-2805.