发展了Yb(OTf)3催化的碳氢键活化2-甲基氮杂芳烃或4-甲基氮杂芳烃对靛红的加成反应,对不同靛红和氮杂芳烃都取得了较好的产率.该方法能够一步快速合成具有重要生理活性的氮杂芳烃取代的3-羟基-2-氧化吲哚类化合物,同时该反应成功扩展了路易斯酸在sp3碳氢键活化中的应用.
3-Substituted-3-hydroxy-2-oxindoles are rich in a range of biologically active natural products and pharmaceuticals and development of efficient methods to construct this key motif is of vital importance.Yb(OTf)3-catalyzed addition of 2-or 4-methyl azaarenes to isatins via C-H functionalization was developed.Moderate to good yields were obtained for various isatins and azaarenes.This method provides rapid protocol for the synthesis of biologically important azaarene-substituted 3-hydroxy-2-oxindoles in one step.The success of this reaction expands the synthetic utility of Lewis acid in the catalytic functionalization of sp3 C-H bonds in organic synthesis.