Polymer-supported quenching reagents for parallel purification

被引:263
作者
Booth, RJ [1 ]
Hodges, JC [1 ]
机构
[1] PARKE DAVIS PHARMACEUT RES,ANN ARBOR,MI 48105
关键词
D O I
10.1021/ja9634637
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:4882 / 4886
页数:5
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