Polysubstituted pyrrolin-4-ones have been efficiently synthesized from readily available 1-(N- sulfonylazetidin-2-yl) ynones via gold (I)-catalyzed cyclization/nucleophilic substitution in the presence of various nucleophiles, such as water, alcohols, or indoles. Additionally, 3- iodopyrrolin-4-one derivatives have also been obtained under the same reaction conditions upon addition of 1.2 equiv of N-iodosuccinimide.