Palladium‐Catalyzed Hydroamination of Vinyl Ethers with Indoles: Efficient Access to N , O ‐Aminal Indoles

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Indole alkaloids represent a privileged class of natural products with significant potential in drug discovery. Herein, an efficient palladium-catalyzed N-alkylation of indoles with vinyl ethers has been developed. This atom-economic hydroamination demonstrates good functional group tolerance and broad substrate scope across diverse indole alkaloids, providing straightforward access to valuable N,O-aminal indole derivatives. This reaction features mild reaction conditions, complete N1-regioselectivity, operational simplicity, and straightforward product transformation.