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A gold(I)/Brønsted acid‐catalyzed cyclization of 2‐azidobenzaldehydes with 3‐aza‐1,6‐enynes has been developed for the synthesis of tetrahydrobenzo[b][1,8]naphthyridine derivatives. This protocol enabled the modular synthesis of tetracyclic heterocycles in one operation with water and nitrogen gas as the byproducts.
Efficient one-pot transformation of 3-aza-1,5-enynes to poly-substituted pyridines in good to excellent yields has been developed. This reaction involved cyclization of 3-aza-enynes and elimination of sulfinyl acids steps.
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