Transition Metal-Free Synthesis of Substituted Isothiazoles via Three-Component Annulation of Alkynones, Xanthate and NH4I

Article abstract of DOI:10.1002/adsc.202001179

A protocol was described to access diverse isothiazoles with functionalization potential via transition metal-free three-component annulation of alkynones, potassium ethylxanthate (EtOCS₂K) and ammonium iodide (NH₄I). A sequential regioselective hydroamination/thiocarbonylation/intramolecular cyclization cascade achieved the efficient formation of consecutive C?N, C?S and N?S bonds in a one-pot process. (Figure presented.).