Abstract

A new one-pot and regioselective synthesis of functionalized γ-lactams by a metal-free Ugi 4CR/intramolecular 5-exo-dig cyclization sequence under mild conditions has been developed. The reaction of propenoic acids, aldehydes, amines, and isocyanides produced γ-lactams regioselectively in 72–89% yields via sequential Ugi 4CR/intramolecular 5-exo-dig cyclization reaction in the presence of Cs2CO3.

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