State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University , Changsha 410082, P. R. China.
State Key Laboratory of Anti-Infective Drug Development (NO. 2015DQ780357), Sunshine Lake Pharma Co., Ltd , Dongguan 523871, P. R. China.
J Org Chem. 2017 Jun 2;82(11):5810-5818. doi: 10.1021/acs.joc.7b00633. Epub 2017 May 23.
A general and direct N-arylation of sulfonamides and NH-sulfoximines by sodium arylsulfinates through a desulfitative pathway was herein demonstrated. The reaction proceeded with catalytic loadings of Cu(II)-catalysts without any external ligands. And the novel arylation protocol featured for high efficiency (up to 93% yields) and good substituent tolerance (up to 53 examples). Moreover, a plausible reaction mechanism was also discussed.
本文展示了通过脱硫途径，利用苯磺酸钠将磺胺和 NH-亚磺酰胺进行一般性和直接的 N-芳基化。该反应在没有任何外部配体的情况下，使用催化量的 Cu(II)-催化剂进行。该新的芳基化方案具有高效（最高收率达 93%）和良好的取代基耐受性（多达 53 个实例）的特点。此外，还讨论了一个合理的反应机制。
