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A photoredox-catalyzed direct difluoromethylation of alkynoates has been developed. A well-designed photoredox system induces a single-step, regioselective installation of CF2H onto alkynes. Difluoromethyl sulfone was used as an easy to handle CF2H radical source to afford the desired 3-difluoromethylated coumarins in moderate to good yields via a radical-triggered tandem difluoromethylation/5-exo cyclization/ester migration process.

Graphical abstract: Visible-light-mediated direct difluoromethylation of alkynoates: synthesis of 3-difluoromethylated coumarins

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