A facile access to N-sulfonylthioimidates and their use for the transformation to 3,4-dihydroquinazolines

N-Sulfonylthioimidates can be efficiently synthesized through one-pot three-component coupling of terminal alkynes, sulfonyl azides, and thiols by using a copper(i) catalyst in the presence of 4-dimethylaminopyridine. The proposed reaction is characterized by mild reaction conditions and tolerance of diverse functional groups. Additionally, the crucial pharmacophore of 3,4-dihydroquinazolines was synthesized using a one-pot synthetic strategy from N-sulfonylthioimidates.