Aerobic Cu(I)‐Catalyzed Site‐Selective 1,3‐Difunctionalization of Indazole through Cascade C−N and C−O Bond Formation

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A Cu(I)‐catalyzed 1,3 oxo alkylation of indazole has been developed for constructing N ‐1‐alkylated indazolone derivatives. This cascade reaction involves the formation of C−N and C−O bonds through the sequential functionalization of N1 and C3 positions of indazole in 41–89% yields. The photo‐physical studies of the synthesized compounds showed efficient quantum yields with high Stoke shift values. The preliminary experimental results suggest an aerobic manifold of the present protocol through single electron transfer. magnified image