Department of Pharmacy, School of Medicine, Health Science Center, Shenzhen University, Shenzhen 518060, China.
Shenzhen Center for Disease Control and Prevention, Shenzhen 518100, China.
Org Biomol Chem. 2021 Mar 21;19(11):2481-2486. doi: 10.1039/d0ob02444a. Epub 2021 Mar 3.
A novel electrochemical method for the synthesis of α,β-epoxy ketones is reported. With KI as the redox mediator, methyl ketones reacted with aldehydes under peroxide- and transition metal-free electrolytic conditions and afforded α,β-epoxy ketones in one pot (36 examples, 52-90% yield). This safe and environmental-friendly method has a broad substrate scope and can readily provide a variety of α,β-epoxy ketones in gram-scales for evaluation of their anti-cancer activities.
本文报道了一种新颖的电化学方法用于合成α,β-环氧酮。以碘化钾为氧化还原介体，在无过氧化物和过渡金属的电解条件下，甲基酮与醛反应一锅法得到α,β-环氧酮（36 个实例，产率 52-90%）。该方法安全环保，底物适用范围广泛，可以很容易地提供各种克级的α,β-环氧酮，用于评估其抗癌活性。
