Direct Access to 4-Substituted Isoquinolones via a Sequential Pd-Catalyzed Cyclization/Base-Promoted Aromatization/Ring-Opening of N-Propargyl-1,3-oxazolidines

The development atom-economic strategies to construct structurally diverse isoquinolones remains challenging. Herein, we disclose a practical Pd-catalyzed cyclization/base-promoted aromatization/ring-opening protocol of N-propargyl-1,3-oxazolidines with carboxylic acids. In the current domino reaction, a series of ester-functionalized isoquinolones is obtained in moderate to good yields via C−O bond cleavage, which features a broad functional group tolerance. © 2022 Elsevier B.V.