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Dr. Bo Yao, Dr. Qian Wang and Prof. Dr. Jieping Zhu Palladium-Catalyzed Coupling of ortho-Alkynylanilines with Terminal Alkynes Under Aerobic Conditions: Efficient Synthesis of 2,3-Disubstituted 3-Alkynylindoles Angewandte Chemie International Edition 51

Version of Record online: 4 NOV 2012 | DOI: 10.1002/anie.201205596

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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.

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