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Trifluoromethylation/Difluoromethylation‐Initiated Radical Cyclization of o‐Alkenyl Aromatic Isocyanides for Direct Construction of 4‐Cyano‐2‐Trifluoromethyl/Difluoromethyl‐Containing Quinolines
Advanced Synthesis & Catalysis ( IF 5.4 ) Pub Date : 2020-03-18 , DOI: 10.1002/adsc.202000155
Shukuan Mao 1 , He Wang 1 , Lu Liu 1 , Xin Wang 1 , Ming‐Dong Zhou 1 , Lei Li 1
Affiliation  

In this study, a radical‐triggered cyclization of o ‐alkenyl aromatic isocyanides prepared from accessible starting materials is developed. The reaction provides a general and efficient method for the synthesis of 4‐CN‐2‐CF3/CF2H‐containing quinolines under copper or visible‐light photoredox catalysis in a one‐pot synthetic procedure. This protocol demonstrates good to high yields, broad substrate scope, and good functional group tolerance.

中文翻译:

由三氟甲基化/二氟甲基化引发的邻链烯基芳族异氰酸酯的自由基环化反应,可直接构建4-氰基-2-三氟甲基/二氟甲基的喹啉

在这项研究中,开发了由可触及的原料制备的烯基芳族异氰酸酯的自由基触发环化反应。该反应为一锅合成法在铜或可见光光氧化还原催化下合成含4-CN-2-CF 3 / CF 2 H的喹啉提供了一种通用而有效的方法。该协议证明了良好的高产量,广泛的底物范围和良好的官能团耐受性。
更新日期:2020-03-18
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