通过串联米氏反应/脱水序列直接组装异戊烯基化杂芳烃。
Direct Assembly of Prenylated Heteroarenes through a Cascade Minisci Reaction/Dehydration Sequence.
作者信息
Tan Dong-Hang, Zeng Yao-Fu, Liu Yao, Lv Wen-Xin, Li Qingjiang, Wang Honggen
机构信息
School of Pharmaceutical Sciences Sun Yat-sen University Guangzhou 510006 P. R. China.
出版信息
ChemistryOpen. 2016 Oct 11;5(6):535-539. doi: 10.1002/open.201600096. eCollection 2016 Dec.
The prenyl group is an important component in bioactive compounds. Herein, we report the assembly of prenylated heteroarenes through a cascade Minisci reaction and acid-promoted dehydration sequence. The use of potassium (3-hydroxy-3-methylbut-1-yl)trifluoroborate as a new coupling reagent allows the direct introduction of prenyl and 3-hydroxy-3-methylbutyl groups to a wide variety of electron-deficient heteroarenes. Synthetic application is also demonstrated.
异戊二烯基是生物活性化合物中的重要组成部分。在此，我们报道了通过串联的Minisci反应和酸促进的脱水序列来组装异戊二烯基化的杂芳烃。使用(3-羟基-3-甲基丁-1-基)三氟硼酸钾作为一种新的偶联试剂，可以将异戊二烯基和3-羟基-3-甲基丁基直接引入到各种缺电子杂芳烃中。还展示了其合成应用。
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