An operationally simple method for the direct and selective N- and O-difluoromethylation of 2-pyridones, quinoliones, and isoquinolinones with the commercially available TMSCF2Br is described. The chemoselectivity can be tuned by changing reaction temperature, solvents, and bases. Various of functional groups that have reported to be reactive with TMSCF2Br can be tolerated under both conditions. Gram-scale reactions is also performed for both N- and O-difluoromethylation.

Chemoselective N- and O-difluoromethylation of 2-pyridones, isoquinolinones, and quinolinones with TMSCF2Br

ACS Spring 2022

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