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Multicomponent Assembly of Highly Substituted Indoles by Dual Palladium-Catalyzed Coupling Reactions


  • We thank the National Institute of Health (GM089153), the National Science Foundation (CHE-0910870 and CHE-030089 with the Pittsburgh Supercomputer Center) for their generous financial support. We also thank Prof. Annaliese Franz (UC Davis) and Prof. Tomislav Rovis (Colorado State) for helpful discussions.


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Highly substituted indoles were synthesized by a palladium-catalyzed reaction involving three independent components in a one-pot reaction. Two distinct palladium-catalyzed coupling reactions occur with a single catalytic system: a Buchwald-Hartwig reaction and an arene-alkene coupling. Quantum chemical computations provide insight into the mechanism of the latter coupling step.