Synthesis of Indolines and Derivatives by Aza-Heck Cyclization
Synthesis of Indolines and Derivatives by Aza-Heck Cyclization
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DOI：
10.1002/anie.201907758
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发表时间：
2019-08-13
影响因子：
16.6
通讯作者：
Watson, Donald A.
中科院分区：
文献类型：
--
作者：
Xu, Feiyang;Korch, Katerina M.;Watson, Donald A.
首次描述了可制备二氢吲哚支架的氮杂赫克环化。该方法使用 N-羟基苯胺作为亲电子试剂，可以很容易地从相应的硝基芳烃中获得，提供带有侧基官能团和复杂环拓扑的二氢吲哚。使用这种方法也可以合成具有挑战性的二氢吲哚，例如在 C2 处具有完全取代的碳原子的二氢吲哚。
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.