Neuroscience Medicinal Chemistry, Research and Development, Janssen Pharmaceutica, Turnhoutseweg 30, 2340 Beerse, Belgium.
J Org Chem. 2012 Mar 16;77(6):2966-70. doi: 10.1021/jo202686p. Epub 2012 Mar 6.
Efficient Csp(3)-Csp(3) Suzuki couplings have been developed with both potassium cyclopropyl- and alkoxymethyltrifluoroborates. Moderate to good yields have been achieved in the cross-coupling of potassium cyclopropyltrifluoroborate with benzyl chlorides possessing electron-donating or electron-withdrawing substituents. Benzyl chloride was also successfully cross-coupled to potassium alkoxymethyltrifluoroborates derived from primary, secondary, and tertiary alcohols.
高效的 Csp(3)-Csp(3)铃木偶联反应已经分别用环丙基和烷氧基甲基三氟化硼酸钾发展起来了。用具有给电子或吸电子取代基的苄基氯与环丙基三氟化硼酸钾的交叉偶联反应得到了中等至良好的产率。苄基氯也成功地与衍生自伯、仲和叔醇的烷氧基甲基三氟化硼酸钾发生了交叉偶联。