Tandem One-Pot Construction of Indoles via Palladium and Copper-Catalyzed Coupling Reactions of the Blaise Reaction Intermediate

[摘要]：The palladium-catalyzed intramolecular N-arylation of the Blaise reaction intermediate, formed by reaction of nitriles with an in situ generated Reformatsky reagent from ethyl alpha-bromo-alpha-(2-bromophenyl)acetate and zinc, afforded indoles in good yields. Extension of this approach to the chemoselective intramolecular N-alkylation/palladium-catalyzed N-arylation of the Blaise reaction intermediate, having omega-chloroalkyl appendages, provided a novel route for the tandem one-pot synthesis of N-fused indole derivatives. In contrast, the intermolecular coupling reaction of the Blaise reaction intermediates with 1,2-dihalobenzene did not proceed in the presence of a palladium catalyst, but proceeded in the presence of copper(I) iodide as the catalyst and resulted in indoles.

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