An efficient copper‐catalyzed tandem strategy for the construction of triazole‐fused polycyclic quinazolinone frameworks has been developed. This methodology is accomplished through a multicomponent protocol involving 2‐bromophenyl quinazolinones, sodium azide, and terminal alkynes and proceeds via copper‐catalyzed azide–alkyne cycloaddition (CuAAC), Ullmann‐type C—N coupling, and intramolecular C—N bond formation, delivering quinazolino3,2‐ c 1,2,3 triazolo1,5‐ a quinazolin‐14‐ones in 60%–78% yields. Current protocol provides a concise and valuable route for constructing structurally complex polycyclic N‐heterocycles with potential pharmaceutical relevance.
Kandula et al. (Thu,) studied this question.