芳基胺的液相合成及其通过亲核芳基取代反应在苯并咪唑酮中的应用。
Liquid phase synthesis of arylamines and its application to the benzimidazolone via nucleophilic aryl substitution.
作者信息
Pan P C, Sun C M
机构信息
Department of Chemistry, National Dong Hwa University, Hualien, Taiwan.
出版信息
Bioorg Med Chem Lett. 1999 Jun 7;9(11):1537-40. doi: 10.1016/s0960-894x(99)00231-0.
A method for soluble, inexpensive polymer-supported synthesis of aryl amines and benzimidazolone on the basis of nucleophilic aryl substitution (S(N)Ar) is described. This method involves a direct coupling reaction between resin bound aryl fluoride and amines at ambient temperature. The products are isolated in quantitative yields and excellent purity by simple precipitation and washing. This liquid phase method proves to be a useful tool for constructing combinatorial arylamine and benzimidazolone libraries.
描述了一种基于亲核芳基取代（S(N)Ar）的可溶性、低成本聚合物负载合成芳基胺和苯并咪唑酮的方法。该方法涉及在环境温度下树脂负载的芳基氟化物与胺之间的直接偶联反应。通过简单的沉淀和洗涤，产物以定量产率和优异的纯度分离出来。这种液相方法被证明是构建组合芳基胺和苯并咪唑酮文库的有用工具。
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