Boron Trichloride‐Mediated Synthesis of Indoles via the Aminoboration of Alkynes,Advanced Synthesis & Catalysis

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Boron Trichloride‐Mediated Synthesis of Indoles via the Aminoboration of Alkynes
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-09-07 , DOI: 10.1002/adsc.201800509
Jiahang Lv _{1,

2} , Binlin Zhao ₂ , Li Liu ₃ , Ying Han ₁ , Yu Yuan ₁ , Zhuangzhi Shi _{1,

2}

Affiliation

We describe an efficient catalyst‐ and metal‐free aminoboration of alkynes to 3‐borylated indoles using one of the least expensive boron sources, BCl₃. The major dichloro(indolyl)borane products can be used for the in situ construction of useful 3‐Bpin indoles. This simple and mild method provides a novel and efficient approach for the synthesis of various 3‐borylated indoles with high regioselectivity and a wide substrate scope.

中文翻译：

三氯化硼通过炔烃的氨基硼酸酯化介导的吲哚合成

我们描述了使用最便宜的硼源之一BCl ₃将炔烃有效地进行无催化剂和金属的氨基硼酸酯化，使其生成3硼化的吲哚。主要的二氯（吲哚基）硼烷产品可用于原位构建有用的3-Bpin吲哚。这种简单温和的方法为合成具有高区域选择性和宽底物范围的各种3硼化的吲哚提供了一种新颖而有效的方法。

更新日期：2018-09-07

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