3-Amino-2-oxindole derivatives are a common framework found in many natural products and medicinal compounds and thus their synthesis is of significant importance. We report for the first time a one-pot approach for the synthesis of these compounds, using a bory­lation/intramolecular asymmetric arylation sequence starting from ­ortho-bromo-α-ketimino amide derivatives. Pd(OAc)2 was used as the pre-catalyst along with (R)-BINAP as the chiral source. We successfully obtained a family of 3-phenyl-3-(aryl-amino)-indolin-2-one derivatives (11 in total) with excellent yields (up to 98%) and enantioselectivities of up to 76% ee. The reaction is versatile and tolerant of a wide range of functional groups.

中文翻译：

---

Pd 催化的一锅硼酸化/分子内不对称芳基化在 α-酮亚胺上：手性 3-氨基-2-羟吲哚的创新方法

3-Amino-2-oxindole 衍生物是许多天然产物和药用化合物中常见的骨架，因此它们的合成具有重要意义。我们首次报告了合成这些化合物的一锅法，使用从邻溴-α-酮亚氨基衍生物开始的硼酸化/分子内不对称芳基化序列。Pd(OAc)2 用作预催化剂，(R)-BINAP 用作手性源。我们以优异的产率（高达 98%）和高达 76% ee 的对映选择性成功获得了一系列 3-苯基-3-（芳基-氨基）-indolin-2-one 衍生物（共 11 个）。该反应是通用的，并且可以耐受范围广泛的官能团。