Abstract

AbstractWe report a unique and expeditious route to synthesize 1‐isochromanone derivatives through palladium catalyzed tandem Heck coupling/6‐endo hydroacyloxylation cyclization between readily available ortho‐halogenated benzoates and unactivated alkenes. Various 2‐bromo or 2‐iodo benzoates can be coupled efficiently with a broad range of alkenes to afford functionalized 1‐isochromanones in high yields. Significantly, this cost‐efficient and easy‐to‐handle synthetic methodology will have great prospect application in the synthetic and medicinal chemistry.magnified image

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