Department of Chemistry and Biochemistry, University of Delaware, Newark, DE, 19716, USA.
Angew Chem Int Ed Engl. 2019 Sep 16;58(38):13448-13451. doi: 10.1002/anie.201907758. Epub 2019 Aug 13.
For the first time, an aza-Heck cyclization that allows the preparation of indoline scaffolds is described. Using N-hydroxy anilines as electrophiles, which can be easily accessed from the corresponding nitroarenes, this method provides indolines bearing pendant functionality and complex ring topologies. Synthesis of challenging indolines, such as those bearing fully substituted carbon atoms at C2, is also possible using this method.
首次描述了一种aza-Heck 环化反应，该反应可用于制备吲哚啉骨架。该方法使用 N-羟基苯胺作为亲电试剂，这些亲电试剂可从相应的硝基芳烃中轻易获得，因此该方法可以制备带有侧链官能团和复杂环拓扑结构的吲哚啉。使用该方法还可以合成具有挑战性的吲哚啉，例如在 C2 位具有完全取代碳原子的吲哚啉。
