Progress in the Asymmetric Dearomatization Reactions of Arenols

Asymmetric dearomatization reactions have been identified as fundamental chemical transformation strategies in organic synthesis for accessing structurally diverse chiral three-dimensional molecules from planar feedstocks. In this domain, the asymmetric dearomatization reactions of arenols have attracted extensive interest due to their potential significance in the synthesis of pharmaceuticals and natural products. However, the inherent difficulty in disrupting aromaticity during the dearomatization process creates a significant barrier to the development of such a reaction. Moreover, the competition from side reactions, including electrophilic O-functionalization and Friedel–Crafts reaction pathways, presents another challenge for the asymmetric dearomatization reactions of arenols. This Review provides a comprehensive summary of the progress in asymmetric dearomatization reactions of arenols, highlighting the extraordinary ability of such methodologies in organic synthesis and indicating their limitations and future trends.