We developed iridium-catalyzed 2-position-selective C–H borylation of indole derivatives by modifying the structure of a bipyridine-type ligand. The yields ranged from good to excellent, even on a gram scale, and were dramatically improved by the addition of a urea derivative catalyst. The introduced boryl group was converted to chloro, bromo, and phenyl groups without isolation of the borylated intermediate. Preliminary results indicated the importance of hydrogen bonding between the substrate and the urea additive.

中文翻译：

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尿素加速铱催化的吲哚衍生物的2-位选择性CH硼化

我们通过修饰联吡啶型配体的结构开发了铱催化的吲哚衍生物的2位选择性C–H硼氢化。甚至在克规模上，收率从好到坏不等，并且通过添加脲衍生物催化剂而大大提高了收率。引入的硼基被转化为氯，溴和苯基，而没有分离出硼化的中间体。初步结果表明，底物与尿素添加剂之间氢键的重要性。