Beilstein Arch. 2026, 202644. https://doi.org/10.3762/bxiv.2026.44.v1
Published 12 Nov 2026
Azetidine motifs are valuable for the synthesis of a wide range of biologically active molecules and drug candidates. We report the construction of 3-functionalized azetidines through hypervalent iodine–mediated fluoroamination using pyridine·HF. Two complementary protocols enable simultaneous C–F and C–N bond formation under simple conditions. The reaction tolerates a broad range of N-protected 2-aryl allylamines, affording fluorinated azetidines in moderate-to-good yields.
Keywords: Azetidine, Hypervalent Iodine, fluoroamination
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Lim, N.; Lee, J.; Kim, J. H.; Kang, N. S.; Hong, K. B.; Choi, S. Beilstein Arch. 2026, 202644. doi:10.3762/bxiv.2026.44.v1
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