Enantioselective Allylation of 2,3‐Dioxopyrrolidines via Synergistic Bi(OAc) ₃ /Chiral Phosphoric Acid Catalysis

A highly asymmetric allylation of dioxopyrrolidines with allylboronates is achieved using a Bi(OAc) 3 /chiral phosphoric acid (CPA) catalytic system under mild conditions. This reaction features a broad substrate scope with respect to dioxopyrrolidines, enabling rapid access to a diverse array of chiral 3‐hydroxypyrrolidin‐2‐ones with satisfactory outcomes (up to 99% yields and 94% ee). The synthetic utility of this protocol is demonstrated through gram‐scale reaction and subsequent product transformations. Furthermore, several chiral 3‐hydroxypyrrolidin‐2‐ones show promising antitumor activity against multiple cancer cell lines, highlighting the value of this methodology. Additionally, the reaction mechanism is preliminarily investigated through control experiments and density functional theory (DFT) calculations.