Tandem reaction of heterocyclic ketene aminals with diazoesters: Synthesis of pyrimidopyrrolidone derivatives

A tandem reaction of heterocyclic ketene aminals (HKAs) with diazoesters in the presence of a Cu catalyst is demonstrated for the efficient synthesis of pyrimidopyrrolidone derivatives. The reaction shows a broad substrate scope and excellent functional group tolerance. Our method provides rapid access to diverse pyrimidopyrrolidones in moderate to excellent yields under mild reaction conditions.