A Fluorescence-Based Assay for High-Throughput Screening of Coupling Reactions. Application to Heck Chemistry
作者:Kevin H. Shaughnessy、Paul Kim、John F. Hartwig
DOI:10.1021/ja983419m
日期:1999.3.1
A new fluorescence-based assay for high-throughput screening of reactions that couple two organic molecules is described. The assay involves reaction of one substrate containing a tethered fluorophore with a second molecule that is attached to a solid support. A successful coupling process is signaled by fluorescence of the solid support, which can be isolated by either simple centrifugation or filtration
描述了一种新的基于荧光的检测,用于对结合两个有机分子的反应进行高通量筛选。该测定涉及一种含有系留荧光团的底物与附着在固体支持物上的第二种分子的反应。成功的偶联过程是由固体支持物的荧光发出的信号,可以通过简单的离心或过滤来分离。为了在当前激烈的研究中在催化过程的背景下评估该测定,我们寻找改进的、易于获得的膦用于 Heck 化学。将含有系链香豆素的丙烯酸酯与负载在交联聚苯乙烯树脂上的芳基卤反应。将我们基于荧光的测定结果与连续 GC 分析的结果进行比较表明,基于荧光的测定准确地选择了最活跃的配体,用于芳基溴化物和氯化物的 Heck 偶联。测定选择的两个配体,三(叔丁基)膦和二(叔丁基膦)...