A Cu/Pd-catalyzed tandem radical cyclization and carbonylation of alkyne-tethered α-bromocarbonyls with phenols has been developed for the expedited construction of ester-containing 3,4-dihydroquinolin-2(1)-one scaffolds. By employing benzene-1,3,5-triyl triformate (TFBen) as the CO source, the reaction proceeded smoothly to afford a series of ester-containing 3,4-dihydroquinolin-2(1)-one derivatives in high yields. Moreover, this method could be utilized in the late-stage modifications of bioactive molecules.
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