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Copper-Catalyzed Domino Cycloaddition/C[BOND]N Coupling/Cyclization/(C[BOND]H Arylation): An Efficient Three-Component Synthesis of Nitrogen Polyheterocycles


  • We thank Prof. Stephen L. Buchwald (Massachusetts Institute of Technology) for insightful discussions and Dr. Iain Campuzano (Amgen) for supplying HRMS data. H.W. thanks Amgen Therapeutic Discovery for financial aid during a summer internship.


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A cat of all trades: A single copper catalyst promoted up to three reaction steps with separate catalytic cycles in a domino sequence (azide–alkyne cycloaddition/Goldberg amidation/Camps cyclization/(C[BOND]H arylation)) for the rapid construction of complex heterocycles from three simple components under mild conditions (see scheme). Facile cleavage of the triazole ring enables further elaboration of the condensation products.