Hu Jinhui, Hong Huanliang, Qin Yongwei, Hu Yunfei, Pu Suyun, Liang Gen, Huang Yubing
School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529090, P. R. China.
Org Lett. 2021 Feb 5;23(3):1016-1020. doi: 10.1021/acs.orglett.0c04218. Epub 2021 Jan 21.
A practical protocol has been established to access diverse oxazol-2-amine derivatives in one step via the electrochemical desulfurative cyclization of isothiocyanates and α-amino ketones. On the basis of the cycle of in situ generation of iodine/desulfurative cyclization/iodide anion regeneration, the reaction is performed under metal-free and external-oxidant-free electrolytic conditions to achieve the formation of intermolecular C-O and C-N bonds, providing oxazol-2-amines in moderate to excellent yields.
已建立了一种实用的方案,通过异硫氰酸酯和α-氨基酮的电化学脱硫环化一步合成多种恶唑-2-胺衍生物。基于碘原位生成/脱硫环化/碘离子再生的循环,该反应在无金属和无外部氧化剂的电解条件下进行,以实现分子间C-O和C-N键的形成,从而以中等至优异的产率提供恶唑-2-胺。