"一锅法"钯催化喹啉 N-氧化物区域选择性酰化合成 8-酰基-2-喹啉酮
"One-Pot" Approach to 8-Acylated 2-Quinolinones via Palladium-Catalyzed Regioselective Acylation of Quinoline N-Oxides.
机构信息
Department of Chemistry, Henan Key Laboratory of Chemical Biology and Organic Chemistry, Key Laboratory of Applied Chemistry of Henan Universities, Zhengzhou University , Zhengzhou 450052, P. R. China.
Xiamen Key Laboratory of Ocean and Gene Drugs, School of Biomedical Sciences, Institute of Molecular Medicine of Huaqiao University & Engineering Research Centre of Molecular Medicine of Chinese Education Ministry , Xiamen, Fujian 361021, P. R. China.
出版信息
Org Lett. 2016 May 20;18(10):2411-4. doi: 10.1021/acs.orglett.6b00923. Epub 2016 May 6.
A "one-pot" facile and efficient protocol for 8-acylated 2-quinolinones has been developed through palladium-catalyzed acylation of quinoline N-oxides, which proceeds with high selectivity at the C8-position. The desired products were isolated in up to 95% yield and good functional group tolerance. A palladacycle was isolated from the catalytic process and proposed as a key intermediate.
一种“一锅法”简便高效的 8-酰基-2-喹啉酮合成方法已经通过钯催化的喹啉 N-氧化物酰化反应得以实现，该方法对 C8 位具有高选择性。目标产物的收率高达 95%，且官能团耐受性良好。从催化过程中分离得到了一个钯环配合物，并被提出作为关键中间体。
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