School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Molecules. 2020 Mar 9;25(5):1233. doi: 10.3390/molecules25051233.
We developed an efficient method for synthesis of substituted -benzoylindole via Pd(II)-catalyzed C-H functionalization of substituted -(2-allylphenyl)benzamide. The reaction showed a broad substrate scope (including -acetyl and -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 -benzoylindole over benzoxazine, and this is the first example of Pd(II)-catalyzed synthesis of substituted -benzoylindole. Notably, this new method was applied for the synthesis of key intermediate of indomethacin.
我们开发了一种通过 Pd(II)催化取代的-(2-烯丙基苯基)苯甲酰胺的 C-H 功能化来合成取代的苯甲酰基吲哚的有效方法。该反应具有广泛的底物范围（包括 -乙酰基和 -Ts 底物），并以良好到优秀的收率得到取代的吲哚。该方法的最显著特点是对苯甲酰基吲哚相对于苯并恶嗪具有高选择性，这是首例 Pd(II)催化合成取代的苯甲酰基吲哚的例子。值得注意的是，这种新方法被应用于吲哚美辛的关键中间体的合成。
