Wang Xing, Liu Fu-Di, Tu Hai-Yang, Zhang Ai-Dong
Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University , Wuhan 430079, People's Republic of China.
J Org Chem. 2014 Jul 18;79(14):6554-62. doi: 10.1021/jo5010185. Epub 2014 Jul 8.
A one-pot palladium-catalyzed synthesis of symmetrical and unsymmetrical diarylmethanones using acetophenone and aryl bromides as raw materials has been developed. In this reaction, acetophenone acts as a latent carbonyl donor and two pathways of palladium-catalyzed sequential coupling and aerobic oxidation are identified. The reaction is applicable to a spectrum of substrates and delivers the products in moderate to good yields. This method can be used for the synthesis of ketoprofen, a nonsteroidal anti-inflammatory drug, in a two-step procedure and 45% overall yield.
已开发出一种以苯乙酮和芳基溴为原料，一锅法钯催化合成对称和不对称二芳基甲酮的方法。在该反应中，苯乙酮作为潜在的羰基供体，确定了钯催化的顺序偶联和有氧氧化两条途径。该反应适用于一系列底物，产物收率中等至良好。该方法可用于分两步合成非甾体抗炎药酮洛芬，总收率为45%。
