铜催化吲哚的直接 C6-芳基化反应。
Cu-Catalyzed Direct C6-Arylation of Indoles.
机构信息
State Key Laboratory of Coordination Chemistry, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University , Nanjing 210093, China.
State Key Laboratory and Institute of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering, Nankai University , Tianjin 300071, China.
出版信息
J Am Chem Soc. 2016 Jul 20;138(28):8734-7. doi: 10.1021/jacs.6b05777. Epub 2016 Jul 7.
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.
首次报道了吲哚 C6 位的直接、位点选择性芳基化反应。这种高区域选择性的关键在于选择合适的 N-P(O)(t)Bu2 导向基团，并在催化氧化铜的存在下使用二芳基碘鎓三氟甲磺酸酯盐作为偶联试剂。该反应体系温和，避免使用配体和添加剂，具有广泛的吲哚和芳烃偶联组分，同时保持了其效率和可扩展性，因此在吲哚区域选择性直接芳基化反应的实施方面取得了重大进展。
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