School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, China.
Org Biomol Chem. 2020 Aug 5;18(30):5832-5837. doi: 10.1039/d0ob01163k.
A novel electrochemical synthesis protocol has been achieved for reductive amination between aldehydes and amines in undivided cells at room temperature. Under metal-free and external-reductant-free electrolysis conditions, various important secondary amine products are obtained in moderate-to-high yields. Deuterium-labeling experiments have demonstrated that low-toxicity DMSO acts both as a solvent and a H-donor in the reaction. On this basis, various deuterium-labeled products with good-to-excellent D-incorporation have been synthesized by using DMSO-d6 as a solvent. Furthermore, a molecule with GR-antagonistic activity has been synthesized through further sulfonylation.
一种新型的电化学还原胺化方法在室温下于未分隔的电池中实现了醛和胺之间的还原胺化。在无金属和无外加还原剂的电解条件下，各种重要的仲胺产物以中等至高产率获得。氘标记实验表明，低毒 DMSO 既作为溶剂又作为反应中的 H 供体。在此基础上，通过使用 DMSO-d6 作为溶剂，合成了各种具有良好至优异 D 掺入的氘标记产物。此外，通过进一步磺化合成了具有 GR 拮抗活性的分子。
