Abstract

An efficient synthetic approach for the synthesis of 5‐bromo/iodo‐cyclopentenones containing a C–X (Br, I) stereocenter that relies on gold(I)‐catalyzed cycloisomerization–electrophilic halogenation sequence of 1,3‐enyne esters with N‐bromosuccinimide (NBS) or N‐iodosuccinimide (NIS) is described. This tandem transformation exhibited a broad substrate scope and excellent functional group compatibility, providing a novel protocol for rapid assembly 5‐bromo/iodo‐cyclopentenones in good to excellent yields under mild reaction conditions.

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