Palladium‐Catalyzed Regioselective Synthesis of 1‐Benzoazepine Carbonitriles from o ‐Alkynylanilines via 7‐ endo ‐dig Annulation and Cyanation

We herein report a three‐component, one‐pot cascade reaction involving an imination/annulation/cyanation sequence for the synthesis of 1‐benzoazepine carbonitrile derivatives using readily available o ‐alkynylanilines, cyclic ketones and trimethylsilyl cyanide. This regio‐ and stereoselective reaction was achieved by combining palladium(II) trifluoroacetate and copper(II) acetate in dimethyl sulfoxide. The important features of this method include a broad substrate scope, the use of trimethylsilyl cyanide as a cyanating agent, the formation of two C−C bonds and one C−N bond, mild reaction conditions and good product yields.