Multicomponent Assembly of 1,2,3-Dithiazole-5-thiones via Triple Sulfur Donor Integration

Herein, we report that a metal-free multicomponent strategy integrates Kornblum oxidation, dehydrative condensation, Willgerodt-Kindler-type polysulfuration, and heterocyclization, enabling the synthesis of bioactive 1,2,3-dithiazole-5-thione scaffolds from readily accessible methyl ketones, elemental sulfur, and cyanamides. In this protocol, S8 serves as the triple sulfur donor for both the C═S and ─S2─ moieties, while cyanamides provide the nitrogen source. Remarkably, this method accomplishes the cleavage of triple Csp3─H bonds and the formation of multiple C─heteroatom bonds within one step.