Department of Chemistry, Innovative Drug Research Center, Shanghai University , Shangda Road 99, Shanghai 200436, China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zuchongzhi Road, Shanghai 201203, China.
Org Lett. 2017 Apr 7;19(7):1780-1783. doi: 10.1021/acs.orglett.7b00549. Epub 2017 Mar 23.
A mild and efficient synthesis of N-substituted-2-fluoroindole derivatives was achieved via Buchwald-Hartwig couplings and a sequential, base-promoted intramolecular nucleophilic reaction-β-fluorine elimination. By employing easily obtained gem-difluorostyrenes and primary arylamines, the scope, advantages, and limitations of this reaction were well investigated. Furthermore, this strategy distinguishes itself by high modularity, operational simplicity, and a wide substrate scope, giving rise to a broad array of 2-fluoroindole derivatives in moderate to excellent yields.
通过 Buchwald-Hartwig 偶联反应和顺序的、碱促进的分子内亲核反应- β-氟消除反应，实现了 N-取代-2-氟吲哚衍生物的温和高效合成。通过使用易得的偕二氟苯乙烯和伯芳基胺，对该反应的范围、优点和局限性进行了深入研究。此外，该策略具有高度的模块化、操作简单和广泛的底物范围的特点，在中等至优异的收率下得到了一系列 2-氟吲哚衍生物。
