Zhao Fei, Zhang Dengyou, Nian Yong, Zhang Lei, Yang Wei, Liu Hong
State Key Laboratory of Drug Research, CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zuchongzhi Road, Shanghai 201203, P. R. China.
Org Lett. 2014 Oct 3;16(19):5124-7. doi: 10.1021/ol5024745. Epub 2014 Sep 23.
Palladium-catalyzed intramolecular addition of C-N and S-N bond to alkynes with the migration of functional groups has been achieved. A wide range of functional groups including acyl, pyruvoyl, amide, and sulfonyl groups can migrate smoothly and be conveniently introduced at the C-3 postion of indoles in our catalytic system. The operational simplicity and broad substrate scope demonstrate the great potential of this method for the synthesis of highly functional indoles.
已实现钯催化的分子内C-N和S-N键与炔烃加成并伴随官能团迁移。在我们的催化体系中，包括酰基、丙酮酰基、酰胺和磺酰基在内的多种官能团都能顺利迁移，并方便地引入到吲哚的C-3位。操作简便以及底物范围广泛表明了该方法在合成高官能化吲哚方面的巨大潜力。
