A simple and efficient strategy for the preparation of 3‐acylindoles via palladium‐catalyzed cyclization reaction of N‐(2‐haloaryl)alkynylimines in water has been developed. The reaction tolerates a wide range of functional groups, and the corresponding 3‐acylindoles were obtained in high yields using water as the sole solvent and oxygen sources. Additionally, this method could provide a short synthesis route for Pravadoline, a phase II analgesic drug.
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