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首页> 外文期刊>Journal of combinatorial chemistry >Optimization of three- and four-component reactions for polysubstituted piperidines: Application to the synthesis and preliminary biological screening of a prototype library
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Optimization of three- and four-component reactions for polysubstituted piperidines: Application to the synthesis and preliminary biological screening of a prototype library

机译：多取代哌啶三组分和四组分反应的优化：在原型库的合成和初步生物学筛选中的应用

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摘要

Several solid- and solution-phase strategies were evaluated for the preparation of libraries of polysubstituted piperidines of type 7 using the tandem aza[4+2]cycloaddition/allylboration multicomponent reaction between 1-aza-4-boronobutadienes, maleimides, and aldehydes. A novel four-component variant of this chemistry was developed in solution phase, and it circumvents the need for pre-forming the azabutadiene component. A parallel synthesis coupled with compound purification by HPLC with mass-based fraction collection allowed the preparation of a library of 944 polysubstituted piperidines in a high degree of purity suitable for biological screening. A representative subset of 244 compounds was screened against a panel of phosphatase enzymes, and despite the modest levels of activity obtained, this study demonstrated that piperidines of type 7 display the right physical properties (e.g., solubility) to be assayed effectively in high-throughput enzymatic tests.
机译：使用1-aza-4-boronobutadienes，马来酰亚胺和醛类之间的串联aza [4 + 2]环加成/烯丙基化多组分反应，评估了几种固相和溶液相策略，用于制备7型多取代哌啶的文库。在溶液相中开发了这种化学反应的新型四组分变体，它避免了预先形成氮杂丁二烯组分的需要。平行合成与通过基于质量的馏分收集的HPLC化合物纯化相结合，可以制备944种多取代的哌啶文库，该文库具有适合生物筛选的高纯度。针对一组磷酸酶筛选了244种化合物的代表性子集，尽管获得了适度的活性水平，但这项研究表明，7型哌啶具有正确的物理性质（例如，溶解度），可在高通量下进行有效分析酶测试。

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