Efficient Synthesis of Fluoroalkylated Imidazoles via a Metal‐Free Cascade Michael Addition/Azidation/Cycloamination Process

In the presence of KI and (diacetoxyiodo)benzene (PIDA), primary amines bearing an α‐hydrogen can be efficiently converted to fluoroalkylated imidazoles by reacting with fluoroalkylated alkynes and sodium azide via a cascade Michael addition/azidation/cycloamination process. KI plays a crucial role in this reaction by generating iodine(I) species to promote the cyclization. Substrate scope was explored, and the application of this protocol was demonstrated. Additionally, a plausible reaction mechanism was proposed.