ELTE "Lendület" Catalysis and Organic Synthesis Research Group, Institute of Chemistry, Eötvös Loránd University, Pázmány Péter stny. 1/A, 1117, Budapest, Hungary.
Innostudio Inc., Záhony u. 7, 1031, Budapest, Hungary.
Chemistry. 2022 Apr 6;28(20):e202103967. doi: 10.1002/chem.202103967. Epub 2022 Feb 14.
DNA-encoded library (DEL) technology has become widely used in drug discovery research. The construction of DELs requires robust organic transformations that proceed in aqueous media under mild conditions. Unfortunately, the application of water as reaction medium for organic synthesis is not evident due to the generally limited solubility of organic reagents. However, the use of surfactants can offer a solution to this issue. Oil-in-water microemulsions formed by surfactant micelles are able to localize hydrophobic reagents inside them, resulting in high local concentrations of the organic substances in an otherwise poorly solvated environment. This review provides a conceptual and critical summary of micellar synthesis possibilities that are well suited to DEL synthesis. Existing examples of micellar DEL approaches, together with a selection of micellar organic transformations fundamentally suitable for DEL are discussed.
DNA 编码文库 (DEL) 技术已广泛应用于药物发现研究。DEL 的构建需要在温和条件下在水介质中进行稳健的有机转化。不幸的是，由于有机试剂的溶解度通常有限，水作为有机合成的反应介质的应用并不明显。然而，表面活性剂的使用可以解决这个问题。由胶束形成的油包水乳状液能够将疏水性试剂定位在其中，从而在 otherwise 溶解度差的环境中，在有机物质的局部浓度很高。这篇综述提供了一个概念和批判性的总结，适用于 DEL 合成的胶束合成可能性。讨论了现有的胶束 DEL 方法的例子，以及一些基本适用于 DEL 的胶束有机转化。
