Net Oxidative Photocatalytic Strategy toward the o-Trifluoroacetylation of N-Heteroarenes

Abstract

The direct introduction of fluorinated functional groups into small molecules remains one of the most powerful chemical transformations toward synthesizing biologically active compounds. Heteroaromatics are particularly significant scaffolds, and fluorofunctionalization reactions are still in demand. Herein, we report a protocol to synthesize heteroaromatic trifluoromethyl ketones (TFMKs), installed through photomediated Minisci coupling, followed by subsequent deketalization. We have demonstrated the key Minisci reaction in more than 10 unique heterocyclic classes, notably including pyridines, pyrazines, pyridazines, pyrimidines, quinolines, and polycyclic systems, alongside select deketalizations of high-value aromatics.