TfOH Catalyzed Chemoselective S‐Alkylation of 1 <i>H</i> ‐Tetrazole‐5‐thiones with α‐Diazo Carbonyl Compounds via Formal S–H Insertion

Abstract A metal‐free, TfOH‐catalyzed S‐alkylation of tetrazole‐5‐thiones using diazo carbonyl compounds through formal S–H insertion has been disclosed. This new methodology offers simple, mild, and efficient access to chemoselective S‐alkylation of tetrazole‐5‐thiones in a short reaction time. Further, various diversely substituted acceptor and donor/acceptor‐type diazo carbonyl compounds smoothly deliver the expected product with high chemoselectivity.