分子内、位点选择性、碘介导的未活化(sp)C-H 键胺化反应在吲哚衍生物合成中的应用。
Intramolecular, Site-Selective, Iodine-Mediated, Amination of Unactivated (sp)C-H Bonds for the Synthesis of Indoline Derivatives.
机构信息
State Key Laboratory of Chemo/Biosensing and Chemometrics,College of Chemistry and Chemical Engineering, Hunan University , Changsha, 410082, China.
Department of Applied Chemistry, Graduate School of Engineering, Osaka University , Suita, Osaka 565-0871, Japan.
出版信息
Org Lett. 2017 Jun 2;19(11):2793-2796. doi: 10.1021/acs.orglett.7b00846. Epub 2017 May 16.
The Iodine-mediated oxidative intramolecular amination of anilines via cleavage of unactivated (sp)C-H and N-H bonds for the production of indolines is described. This transition-metal-free approach provides a straightforward strategy for producing (sp)C-N bonds for use in the preferential functionalization of unactivated (sp)C-H bonds over (sp)C-H bonds. The reaction could be performed on a gram scale for the synthesis of functionalized indolines.
本文描述了一种通过断裂未活化的(sp)C-H 和 N-H 键实现碘介导的苯胺的氧化分子内胺化反应，从而生成吲哚啉的方法。这种无过渡金属的方法为生成(sp)C-N 键提供了一种直接的策略，可用于优先对未活化的(sp)C-H 键进行官能化，而不是对(sp)C-H 键进行官能化。该反应可在克级规模下进行，用于合成功能化的吲哚啉。
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