Fluoroamination of Alkenes Mediated by Hypervalent Iodine to Access 3-Functionalized Azetidines

Abstract

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.

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