posted on 2024-02-07, 14:10authored byJames
A. Vogel, Kirya F. Miller, Eunjeong Shin, Jenna M. Krussman, Patrick R. Melvin
Fluoroformamidines
are an underutilized and understudied functional
group despite combining two of the most highly prized elements in
drug design: nitrogen and fluorine. We report a practical and modular
synthesis of fluoroformamidines via the rearrangement of in
situ-generated amidoximes. High yields in just 60 s at room
temperature highlight the efficiency of this protocol. Furthermore,
fluoroformamidines proved to be useful intermediates in the synthesis
of diverse ureas and carbamimidates.