A practical synthesis of substituted 2,6-diaminopyridines via microwave-assisted copper-catalyzed amination of halopyridines
作者:Matthias Mastalir、Egon E. Rosenberg、Karl Kirchner
DOI:10.1016/j.tet.2015.08.042
日期:2015.10
selective substitution of one or two halogens by aryl or alkylamines was achieved within 2–6 h with temperatures between 80 and 225 °C affording 2,6-diaminopyridines in good to excellent isolated yields. The reaction allows easy variation between educts and different N-substitutions. The target compounds are valuable precursors for the synthesis of bis-phosphorylated 2,6-diaminopyridines which are
据报道,利用一系列的2,6-二卤代和2-氨基-6-卤代吡啶前体,进行了微波辅助的铜催化的胺化反应。使用该方法,被芳基或烷基胺一个或两个卤素选择性取代物2-6小时内用80和225之间的温度下℃下,得到良好的2,6-二氨基吡啶,以优异的分离产率来实现的。该反应允许离析物和不同之间容易变化Ñ -substitutions。目标化合物可用于被用作过渡金属络合物PNP钳配体的双-磷酸化2,6-二氨基吡啶合成有价值的前体。