Iron-catalyzed cascade synthesis of nitrogen polycycles from alkynoic acids and functionalized amines

Abstract Catalysis by first-row transition metals is of increasing interest in the context scarcity chemical resources. For instance, iron promising due to its abundance, low toxicity and unique electronic features. Here we synthesized quinazoline alkaloids from alkynoic acids functionalized amines presence dibromide pyridine toluene or, alternatively, a solventless reaction system. We studied sources, media effect additives. Results show 39–99% yields regioselective preparation nitrogen- oxygen-containing scaffolds. This first example cascade process involving catalyzed iron. Fe more abundant, cheaper less toxic than other Au, Cu Ru catalysts previously reported for similar transformations.