Palladium‐Catalyzed Three‐Component Process to [1,2,3]Triazolo [1,5‐c]quinazolines

An efficient palladium‐catalyzed three‐component reaction for the synthesis of tricyclic fused 1,2,3‐triazole derivatives from amino‐NH‐1,2,3‐triazoles, isocyanide and iodoarenes has been developed, involving three new bonds formation by one manipulation in moderate to good yields with excellent functional group tolerance. Moreover, it is also suitable for other N‐heterocyclic substrates including pyrazole, imidazole, indole, tetrazole and its derivatives. Herein we present a facile and efficient three‐component process for the construction of fused 1,2,3‐triazoloquinazoline skeleton in moderate to excellent yields, which tolerates a wide range of functional groups. A scale‐up experiment and derivatizations were also carried out, suggesting the potential utilities of this protocol.