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Assembly of 3-Substituted Isocoumarins via a CuI-Catalyzed Domino Coupling/Addition/Deacylation Process

Shangjun Cai, Fei Wang and Chanjuan Xi*

*Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084, China, Email:

S. Cai, F. Wang, C. Xi, J. Org. Chem., 2012, 77, 2331-2336.

DOI: 10.1021/jo2026433


An efficient strategy for the synthesis of a variety of 3-substituted isocoumarins in very good yields proceeds from o-halobenzoic acids and 1,3-diketones via a copper(I)-catalyzed domino reaction in DMF under the action of K3PO4 at 90-120C without a ligand.

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ID: J42-Y2012-0570