An efficient and mild palladium-catalyzed cascade carboesterification has been developed to afford functionalized α-methylene-γ-lactones in moderate to good yields with high regio- and diastereo-selectivities. Their structures were confirmed by IR, 1H NMR, 13 C NMR and HRMS. Furthermore, this reaction provided a novel and convenient methodology for the construction of naturally occurring biologically active α-methylene-γ-lactones.
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