利用双硼酸的两步一锅钯催化硼化/Suzuki 交叉偶联反应的范围。
Scope of the two-step, one-pot palladium-catalyzed borylation/Suzuki cross-coupling reaction utilizing bis-boronic acid.
机构信息
Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
出版信息
J Org Chem. 2012 Oct 5;77(19):8678-88. doi: 10.1021/jo301642v. Epub 2012 Sep 20.
Abstract
The use of bis-boronic acid for the direct synthesis of boronic acids has greatly facilitated the two-step, one-pot borylation/Suzuki cross-coupling reaction between aryl and heteroaryl halides. With use of Buchwald's second-generation XPhos preformed catalyst, high yields of cross-coupled products were obtained for most substrates. The method also allows an efficient two-step, one-pot synthesis, providing access to three distinct cross-coupled products after column chromatography. The method also provides a rapid and convenient route to teraryl compounds.
摘要
双硼酸酯在硼酸直接合成中的应用极大地促进了芳基和杂芳基卤化物的两步一锅法硼化/Suzuki 交叉偶联反应。使用 Buchwald 第二代 XPhos 预制催化剂，大多数底物都能获得高产率的交叉偶联产物。该方法还允许进行高效的两步一锅法合成，经柱色谱分离后可获得三种不同的交叉偶联产物。该方法还为合成三联芳烃化合物提供了一种快速便捷的途径。
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