Liang Yujie, Liang Yu-Feng, Tang Conghui, Yuan Yizhi, Jiao Ning
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xue Yuan Rd. 38, Beijing 100191 (P. R. China), Fax: (+86) 10-82805297 http://sklnbd.bjmu.edu.cn/nj/
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xue Yuan Rd. 38, Beijing 100191 (P. R. China), Fax: (+86) 10-82805297 http://sklnbd.bjmu.edu.cn/nj/.
Chemistry. 2015 Nov 9;21(46):16395-9. doi: 10.1002/chem.201503533. Epub 2015 Sep 29.
A cationic cobalt(III)-catalyzed direct C-H amidation of unactivated (hetero)arenes and alkenes by using 1,4,2-dioxazol-5-ones as the amidating reagent has been developed. This transformation proceeds efficiently under external oxidant-free conditions with a broad substrate scope. Moreover, 6-arylpurine compounds, which often exhibit high potency in antimycobacterial, cytostatic, and anti-HCV activities, can be smoothly amidated, thus offering a mild protocol for their late stage functionalization.
已开发出一种阳离子钴（III）催化的未活化（杂）芳烃和烯烃的直接C-H酰胺化反应，该反应使用1,4,2-二恶唑-5-酮作为酰胺化试剂。这种转化在无外部氧化剂的条件下高效进行，底物范围广泛。此外，通常在抗分枝杆菌、细胞抑制和抗丙型肝炎病毒活性方面表现出高效能的6-芳基嘌呤化合物可以顺利地进行酰胺化反应，从而为它们的后期官能团化提供了一种温和的方法。
