The Vilsmeier reagent: a useful and versatile reagent for the synthesis of 2-azetidinones

摘要

(Chloromethylene)dimethylammonium chloride (Vilsmeier reagent), prepared easily from N,N-dimethylformamide and oxalyl chloride or thionyl chloride, works as a versatile acid activator reagent for the direct [2+2] ketene-imine cycloaddition of substituted acetic acid and imines in one-pot synthesis under mild conditions. Monocyclic, spirocyclic and 3-electron-withdrawing group beta-lactams were synthesized by this method and optimization of conditions were performed.