Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
Org Lett. 2012 Aug 17;14(16):4242-5. doi: 10.1021/ol301956p. Epub 2012 Aug 8.
A library of benzimidazole-substituted potassium organotrifluoroborates was prepared via the condensation of various potassium formyl-substituted aryl- and heteroaryltrifluoroborates with aromatic 1,2-diamines under oxidative conditions. The efficient Suzuki-Miyaura cross-coupling of products thus formed to various aryl and heteroaryl bromides was achieved in good yields. The method allows the facile preparation of benzimidazole-containing triaromatic products in two steps from simple potassium formyl substituted aryl- or heteroaryltrifluoroborates.
通过各种钾甲酰基取代的芳基和杂芳基三氟硼酸盐与芳香族 1,2-二胺在氧化条件下缩合,制备了苯并咪唑取代的钾有机三氟硼酸盐库。由此形成的产物与各种芳基和杂芳基溴化物的高效铃木-宫浦交叉偶联反应以良好的产率实现。该方法允许从简单的钾甲酰基取代的芳基或杂芳基三氟硼酸盐以两步法轻松制备含苯并咪唑的三芳基产物。