化学
转鼓
对映选择合成
废止
催化作用
组合化学
药物化学
电泳剂
作者
Peng Yang,Qiang Wang,Bing-Hui Cui,Xiao-Dong Zhang,Hang Liu,Yue-Yuan Zhang,Jia-Liang Liu,Wen-Yu Huang,Ren-Xiao Liang,Yi-Xia Jia
摘要
Enantioselective [3 + 2] annulation of N-heteroarenes with alkynes has been developed via a cobalt-catalyzed dearomative umpolung strategy in the presence of chiral ligand and reducing reagent. A variety of electron-deficient N-heteroarenes, including quinolines, isoquinolines, quinoxaline, and pyridines, and internal or terminal alkynes are employed in this reaction, showing a broad substrate scope and good functionality tolerance. Annulation of electron-rich indoles with alkynes is also developed. This protocol provides a straightforward access to a variety of N-spiroheterocyclic molecules in excellent enantioselectivities (76 examples, up to 99% ee).
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