Center for Drug Discovery, Department of Pathology and Immunology , Baylor College of Medicine , Houston , Texas 77030 , United States.
Bioconjug Chem. 2019 Aug 21;30(8):2209-2215. doi: 10.1021/acs.bioconjchem.9b00447. Epub 2019 Jul 31.
A strategy for DNA-compatible, palladium-catalyzed hydroxycarbonylation of (hetero)aryl halides on DNA-chemical conjugates has been developed. This method generally provided the corresponding carboxylic acids in moderate to very good conversions for (hetero)aryl iodides and bromides, and in poor to moderate conversions for (hetero)aryl chlorides. These conditions were further validated by application within a DNA-encoded chemical library synthesis and subsequent discovery of enriched features from the library in selection experiments against two protein targets.
已开发出一种在 DNA-化学缀合物上对（杂）芳基卤化物进行 DNA 相容钯催化羟羰基化的策略。该方法通常可使（杂）芳基碘化物和溴化物得到中等至非常好的转化，而（杂）芳基氯化物的转化则较差至中等。这些条件通过在 DNA 编码的化学文库合成中的应用以及随后在针对两个蛋白质靶标的选择实验中从文库中发现富集特征得到了进一步验证。
