Cu-Catalyzed Direct C6-Arylation of Indoles.
Cu-Catalyzed Direct C6-Arylation of Indoles.
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DOI：
10.1021/jacs.6b05777
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发表时间：
2016-07
影响因子：
15
通讯作者：
Youqing Yang;Ruirui Li;Yue Zhao;Dongbing Zhao;Zhuangzhi Shi
中科院分区：
文献类型：
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作者：
Youqing Yang;Ruirui Li;Yue Zhao;Dongbing Zhao;Zhuangzhi Shi
报道了第一个在 C6 位点直接和位点选择性芳基化吲哚的例子。这种高区域选择性的关键是正确选择 N-P(O)(t)Bu2 导向基团以及在催化 CuO 存在下使用二芳基碘鎓三氟甲磺酸盐作为偶联配偶体。该方案的特点是温和的反应系统，避免配体和添加剂，表现出广泛的吲哚和芳烃偶联组分，而不影响其效率和可扩展性，从而代表了吲哚区域选择性直接芳基化实施的重大进步。
The first example of direct and site-selective arylation of indoles at the C6 position has been reported. The key to this high regioselectivity is the appropriate choice of the N-P(O)(t)Bu2 directing group and the use of diaryliodonium triflate salts as the coupling partners in the presence of catalytic CuO. The protocol is distinguished by mild reaction system that avoids ligand and additives, exhibiting wide scope of indole and arene coupling components without compromising its efficiency and scalability, thus representing a significant advancement in the implementation of regioselective direct arylation of indoles.