Shen Kun, Wang Qiu
Department of Chemistry , Duke University , Durham , NC 27708-0346 , USA . Email:
Chem Sci. 2017 Dec 1;8(12):8265-8270. doi: 10.1039/c7sc03420b. Epub 2017 Oct 16.
A copper-catalyzed aminoalkynylation of alkenes is achieved with ethynylbenziodoxolone (EBX) reagents under mild conditions with only 1 mol% copper catalyst. This transformation allows for rapid construction of diverse important azahetereocycles and installation of valuable alkyne groups in one step. The developed method features remarkable substrate scope for both terminal and internal alkenes as well as different alkynyl groups, presenting great potential for broad applications in synthesis, bioconjugation, and molecular imaging.
在温和条件下，仅使用1 mol%的铜催化剂，就能实现铜催化的烯烃与乙炔基苯碘酰酮（EBX）试剂的氨基炔基化反应。这种转化能够一步快速构建各种重要的氮杂环，并引入有价值的炔基。所开发的方法对末端烯烃和内烯烃以及不同的炔基都具有显著的底物范围，在合成、生物共轭和分子成像等广泛应用中展现出巨大潜力。
