Biosciences, University of Exeter, Stocker Road, Exeter EX4 4QD, UK.
Org Biomol Chem. 2021 Jan 28;19(3):627-634. doi: 10.1039/d0ob02185g.
A one-pot, three-component protocol for the synthesis of 1,2,3-trisubstituted indoles has been developed, based upon a Fischer indolisation-indole N-alkylation sequence. This procedure is very rapid (total reaction time under 30 minutes), operationally straightforward, generally high yielding and draws upon readily available building blocks (aryl hydrazines, ketones, alkyl halides) to generate densely substituted indole products. We have demonstrated the utility of this process in the synthesis of 23 indoles, benzoindoles and tetrahydrocarbazoles bearing varied and useful functionality.
已经开发出一种基于 Fischer 吲哚化-吲哚 N-烷基化序列的一锅三步法合成 1,2,3-三取代吲哚的方法。该方法非常快速（总反应时间在 30 分钟以内），操作简单，产率通常较高，并且利用易得的构建块（芳基腙、酮、卤代烷）生成多取代的吲哚产物。我们已经证明了该方法在合成具有各种有用官能团的 23 个吲哚、苯并吲哚和四氢咔唑中的实用性。
