Key Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University, Shenzhen Graduate School , Shenzhen, China.
Org Lett. 2013 Oct 18;15(20):5294-7. doi: 10.1021/ol402523x. Epub 2013 Oct 7.
A general protocol for the synthesis of N-alkyl indoles has been developed via a redox neutral C-H activation strategy using a traceless nitroso directing group. A broad scope of substituted N-alkyl indoles has been prepared in good to excellent yields using a very simple Rh catalyst system in the absence of an external oxidant or any other additive. Good to excellent regioselectivity has been achieved for asymmetrically disubstituted acetylenes.
已经开发出一种通过使用无痕迹亚硝基导向基团的氧化还原中性 C-H 活化策略合成 N-烷基吲哚的一般方案。在没有外部氧化剂或任何其他添加剂的情况下，使用非常简单的 Rh 催化剂体系，可以以良好至优异的收率制备广泛的取代 N-烷基吲哚。对于不对称二取代乙炔，实现了良好至优异的区域选择性。
