Stereospecific Electrophilic Fluorocyclization of α,β-Unsaturated Amides with Selectfluor

Org Lett. 2020 Apr 3;22(7):2651-2656. doi: 10.1021/acs.orglett.0c00620. Epub 2020 Mar 16.

Abstract

An efficient fluorocyclization of α,β-unsaturated amides through a formal halocyclization process is developed. The reaction proceeds under transition-metal-free conditions and leads to the formation of fluorinated oxazolidine-2,4-diones with excellent regio- and diastereoselectivity. The evaluation of the reaction mechanism based on preliminary experiments and density functional theory calculations suggests that a synergetic syn-oxo-fluorination occurs and is followed by an anti-oxo substitution reaction. The reaction opens a new window in the field of stereospecific fluorofunctionalization.