A metal-free visible-light-induced decarboxylative radical addition/cyclization procedure at room temperature was described for the synthesis of acylated benzimidazo/indolo[2,1-a]isoquinolines. The procedure was prepared in water via a reaction of functionalized 2-arylbenzoimidazoles or 2,3-diarylindoles and α-oxocarboxylic acids in the presence of phenyliodine(iii) diacetate (PIDA) in one step under mild reaction conditions. In this procedure, traditional heating and metal reagents could be effectively avoided to access 1,4-dicarbonyl-containing benzimidazo/indolo[2,1-a]isoquinoline-6(5H)-ones in satisfactory yields.
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