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  • Title: Assembly of 3-substituted isocoumarins via a CuI-catalyzed domino coupling/addition/deacylation process.
    Author: Cai S, Wang F, Xi C.
    Journal: J Org Chem; 2012 Mar 02; 77(5):2331-6. PubMed ID: 22300252.
    Abstract:
    An efficient strategy for the synthesis of a variety of 3-substituted isocoumarins has been developed. The reaction proceeded from o-halobenzoic acids and 1,3-diketones via a copper(I)-catalyzed domino reaction in DMF under the action of K(3)PO(4) at 90-120 °C without a ligand to afford the corresponding 3-substituted isocoumarin derivatives in good to excellent yields. o-Halobenzoic acids could be o-iodobenzoic acid, o-bromobenzoic acid, and o-chlorobenzoic acid derivatives. 1,3-Diketones could be alkyl- and aryl-substituted 1,3-diketones.
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