Abstract

AbstractAn efficient annulative coupling of benzoic acids with vinyl sulfone is developed based on weak carboxylate‐assisted RuII‐catalyzed ortho C−H bond activation, delivering sulfone containing phthalides in high yields (up to 92 %). The protocol features operational simplicity, mild conditions, and broad substrate scope with wide functional groups tolerance. The synthetic utility was highlighted through the preparation of biologically relevant 3‐ylidenephthalide scaffolds. This work represents the first example of RuII‐catalyzed annulation of benzoic acid with aryl vinyl sulfone.

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