School of Petrochemical Engineering, Changzhou University, Changzhou 213164, P. R. China.
School of Chemistry and Chemical Engineering, Jiangsu University of Technology, Changzhou 213001, P. R. China.
Org Biomol Chem. 2022 Oct 12;20(39):7746-7764. doi: 10.1039/d2ob01463g.
2-Indazoles are one class of the most important nitrogen-containing heterocyclic compounds. The 2-indazole motif is widely present in bioactive natural products and drug molecules that exhibit distinctive bioactivities. Therefore, much attention has been paid to access diverse 2-indazole derivatives. Among them, the late-stage functionalization of 2-indazoles C-H activation is recognized as an efficient approach for increasing the complexity and diversity of 2-indazole derivatives. In this review, we summarized recent achievements in the late-stage functionalization of 2-indazoles, including the C3-functionalization of 2-indazoles through transition metal-catalyzed C-H activation or a radical pathway, transition metal-catalyzed C2'-H functionalization of 2-indazoles and remote C-H functionalization at the benzene ring in 2-indazoles.
2-吲哚类化合物是最重要的含氮杂环化合物之一。2-吲哚基序广泛存在于具有独特生物活性的生物活性天然产物和药物分子中。因此,人们对获得各种 2-吲哚衍生物给予了极大的关注。其中,2-吲哚 C-H 键的后期功能化被认为是增加 2-吲哚衍生物复杂性和多样性的有效方法。在本文中,我们总结了 2-吲哚后期功能化的最新进展,包括通过过渡金属催化 C-H 键活化或自由基途径实现的 2-吲哚 C3-官能化、过渡金属催化的 2-吲哚 C2'-H 官能化以及 2-吲哚苯环的远程 C-H 官能化。