Department of Chemistry, Duke University, Durham, North Carolina, 27708, USA.
Chem Asian J. 2022 Jun 15;17(12):e202200215. doi: 10.1002/asia.202200215. Epub 2022 May 3.
Alkene amino(hetero)arylation presents a highly efficient and straightforward strategy for direct installation of amino groups and heteroaryl rings across a double bond simultaneously. An extensive array of practical transformations has been developed via alkene difunctionalization approach to access a broad range of medicinally valuable (hetero)arylethylamine motifs. This review presents recent progress in 1,2-amino(hetero)arylation of alkenes organized in three different modes. First, intramolecular transformations employing C, N-tethered alkenes will be introduced. Next, two-component reactions will be discussed with different combination of precursors, N-tethered alkenes and external aryl precursor, C-tethered alkenes and external amine precursor, or C, N-tethered reagents, and alkenes. Last, three-component intermolecular amino(hetero)arylation reactions will be covered.
烯键氨基（杂）芳基化反应为同时在双键上直接引入氨基和杂芳基环提供了一种高效而直接的策略。通过烯烃双官能化方法已经开发了广泛的实用转化，以获得广泛的具有药用价值的（杂）芳基乙胺基序。本文综述了以三种不同模式组织的烯烃 1,2-氨基（杂）芳基化的最新进展。首先，将介绍使用 C、N 键合烯烃的分子内转化。接下来，将讨论二组分反应，包括不同的前体组合、N 键合烯烃和外部芳基前体、C 键合烯烃和外部胺前体或 C、N 键合试剂与烯烃。最后，将涵盖三组分分子间氨基（杂）芳基化反应。
