Polymer-supported quenching reagents for parallel purification
Polymer-supported quenching reagents for parallel purification
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DOI：
10.1021/ja9634637
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发表时间：
1997-05-28
影响因子：
15
通讯作者：
Hodges, JC
中科院分区：
文献类型：
--
作者：
Booth, RJ;Hodges, JC
报道了聚苯乙烯-二乙烯基苯支载的三(2-氨基乙基)胺和甲基异氰酸酯衍生物的制备。这些聚合物试剂用于冷却多余的反应物，并从溶液相、尿素、硫脲、磺胺、酰胺和吡唑的平行合成中获得的粗反应产物中去除已知杂质。在反应过程中结合使用其他聚合物反应物，在反应结束时加入聚合物支持的猝灭剂(S)，可以通过一次过滤和挥发溶剂来分离所需的产品。这种方法的机械简单性和效率使快速、并行地提纯通过液相合成获得的粗反应产物成为可能，无论目标产物是单一化合物还是化合物的混合物，因此在组合化学实践中提供了一种有吸引力的固相有机合成的替代方案。
The preparation of polystyrene-divinylbenzene-supported derivatives of tris(2-aminoethyl)amine and methyl isocyanate are described. These polymeric reagents are used to quench excess reactants and remove known impurities from the crude reaction products obtained from the solution-phase, parallel syntheses of ureas, thioureas, sulfonamides, amides, and pyrazoles. In conjunction with the use of other polymeric reactants during the course of a reaction, the addition of polymer-supported quench reagent(s) at the conclusion of the reaction allows isolation of the desired product by a single filtration and evaporation of solvent. The mechanical simplicity and efficiency of this methodology make possible the rapid, parallel purification of crude reaction products obtained via solution-phase syntheses, regardless of whether the intended product is a single compound or a mixture of compounds, and hence offers an attractive alternative to solid-phase organic synthesis in the practice of combinatorial chemistry.