Institute of Biomedical Research, Shandong University of Technology, Zibo, 255000, Shandong, P. R. China.
Zibo Key Laboratory of New Drug Development of Neurodegenerative Diseases, School of Life Sciences and Medicine, Shandong University of Technology, Zibo, 255000, Shandong, P. R. China.
Org Biomol Chem. 2021 Nov 10;19(43):9476-9482. doi: 10.1039/d1ob01807h.
A radical mediated C-H direct formylation of N-heteroarenes with methanol is reported. The reaction features a novel iron-catalyzed Minisci oxidative coupling process using commercially available methanol as a formylating reagent. It effectively solved the long-standing problems associated with using methanol as a formylating reagent in these types of reactions. Compared to the traditional Minisci C-H formylation methods, this protocol is highly atom-economical, simple to operate, and environmentally friendly and shows good functional group tolerance. This Minisci formylation strategy is a straightforward approach for the late-stage functionalization of N-heteroarenes.
报道了一种自由基介导的 N-杂芳环与甲醇的 C-H 直接甲酰化反应。该反应采用了一种新颖的铁催化的 Minisci 氧化偶联过程，使用商业上可获得的甲醇作为甲酰化试剂。它有效地解决了在这些类型的反应中使用甲醇作为甲酰化试剂所带来的长期问题。与传统的 Minisci C-H 甲酰化方法相比，该方法具有高度原子经济性、操作简单、环境友好且对官能团具有良好的耐受性。这种 Minisci 甲酰化策略是 N-杂芳环后期功能化的一种直接方法。
