Tert-Butyl Nitrite Mediated Expeditious Methylsulfoxidation of Tetrazole-amines with DMSO: Metal-free Synthesis of Antifungal Active Methylsulfinyl-1H-tetrazole Derivatives

A tert-butyl nitrite mediated methylsulfoxidation of tetrazole-amines in neat DMSO or methyl-sulfinyl derivatives is revealed for the first time. The reaction exhibits good group tolerance, as well as highly selectivity to sulfinyl substitutions. This new protocol provides an expeditious and operationally simple procedure for C-S(O) bond construction. Preliminary bioactivity evaluation on selected products shows promising antifungal activities.