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Palladium-Catalyzed Coupling of ortho-Alkynylanilines with Terminal Alkynes Under Aerobic Conditions: Efficient Synthesis of 2,3-Disubstituted 3-Alkynylindoles


  • We thank the EPFL (Switzerland), Swiss National Science Foundation (SNSF), and Swiss National Centres of Competence in Research (NCCR) for financial support.


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Two nucleophiles, one triple bond: Under aerobic conditions, palladium-catalyzed direct coupling of o-alkynylanilines and terminal alkynes took place smoothly to afford the 2,3-disubstituted 3-alkynylindoles 3 in good to excellent yields. The intermediate A was characterized and a retro-aminopalladation of B was observed for the first time.