Application of Pd-Catalyzed C–H Alkylation Reaction in Total Syntheses of Twelve Amicoumacin-Type Natural Products

Enantioselective total syntheses of 12 amicoumacin-type natural products are accomplished with a palladium­(II)-catalyzed C–H alkylation as the key step to furnish the 3,4-dihydroisocoumarin scaffold. The target chemicals are assembled in a convergent protocol by merging 3,4-dihydroisocoumarin derived amine part with categories of acid segments that are efficiently prepared by chemoselective catalytic oxidation of chiral 1,2-dihydroxyethylfuran-2­(5H)-ones. Afterward, the cytotoxicity of amicoumacins on five cancer cell lines and one normal cell line is investigated.