Copper-Catalyzed Tandem Reaction of Terminal Alkynes and Sulfonyl Azides for the Assembly of Substituted Aminotriazoles

A simple combination of CuI/LiOtBu/DMF enables the tandem Huisgen [3 + 2] cycloaddition/amidation reaction of terminal alkynes and sulfonyl azides to 5-sulfamide-1-(N-sulfonyl)-1,2,3-triazoles I, which can undergo an alkylation/desulfonation sequence to deliver highly substituted aminotriazoles II by one-pot or one-pot, two-step procedures.