Tandem Friedel−Crafts Alkylation/Lactonization for γ‐Lactone

The lactonization of C(sp3)−H bonds from simple, readily available materials remains a significant challenge in organic synthesis. In this study, we present a tandem Friedel‐Crafts Alkylation /Lactonization reaction using aromatic compounds and cyclo‐anhydrides as raw materials to obtain γ‐lactones under metal‐free conditions. This method offers operational simplicity, broad substrate scope, and high synthetic efficiency. Furthermore, the gram scale experiment of this reaction had been conducted, and the synthesis of natural product Cytosporanone A was achieved using this method.