Herein we describe a practical synthetic method for 3-bromo-2-hydroxy-1-tosylazaindolines and 2-hydroxy-1-tosylazaindoline-3-triethylammonium bromides. 3-Bromo-2-hydroxy-1-tosylazaindolines were found to be stable crystals and could be stored at ambient temperature without consideration of moisture in the air. These indolines are useful reagents for the formal C3-electrophilic reactions of azaindoles with various nucleophiles. We used this method to synthesize various key intermediates of biologically active 3-substituted 7-azaindole derivatives.

中文翻译：

---

3-bromo-2-hydroxy-1-tosylazaindolines的合成与应用

在本文中，我们描述了 3-bromo-2-hydroxy-1-tosylazaindolines 和 2-hydroxy-1-tosylazaindoline-3-triethyl铵溴化物的实用合成方法。发现 3-Bromo-2-hydroxy-1-tosylazaindolines 是稳定的晶体，可以在环境温度下储存，而无需考虑空气中的水分。这些二氢吲哚是用于氮杂吲哚与各种亲核试剂的正式 C3 亲电反应的有用试剂。我们使用这种方法合成了具有生物活性的 3-取代 7-氮杂吲哚衍生物的各种关键中间体。