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We developed an efficient method for synthesis of substituted N -benzoylindole via Pd(II)-catalyzed C-H functionalization of substituted N -(2-allylphenyl)benzamide. The reaction showed a broad substrate scope (including N -acetyl and N -Ts substrates) and substituted indoles were obtained in good to excellent yields. The most distinctive feature of this method lies in the high selectivity for N -benzoylindole over benzoxazine, and this is the first example of Pd(II)-catalyzed synthesis of substituted N -benzoylindole. Notably, this new method was applied for the synthesis of key intermediate of indomethacin.

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Synthesis of Functionalized Indoles via Palladium-Catalyzed Cyclization of N-(2-allylphenyl) Benzamide: A Method for Synthesis of Indomethacin Precursor