A synthetic method of highly substituted quinolines has been developed from N-(2-alkynylaryl)enamine carboxylates under Cu-catalyzed aerobic conditions via intramolecular carbo-oxygenation of alkynes. This strategy was further applied for N-alkynylamidines for amino-oxygenation of alkynes, leading to imidazole and quinazoline derivatives.

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Direct alkenylation of azole heterocycles through Pd–Cu‐catalyzed C–H bond activation has been reported using alkenyl bromides as the coupling partners. The reaction enables the introduction of various mono‐, di‐, or trisubstituted alkenyl bromides as well as a benzyl chloride to the caffeine core.