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A one‐pot approach has been developed for the preparation of a five or six‐membered ring of unsaturated lactones bearing an amino group through a tandem coupling oxacyclization reaction. This tandem process involves Sonogashira‐like cross‐coupling followed by 5‐exo‐dig or 6‐endo‐dig intramolecular oxacyclization, according to the nature of the alkynes substituent. Furthermore, DFT calculations were...
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