Yang Daoshan, Yan Kelu, Wei Wei, Li Guoqing, Lu Shenglei, Zhao Caixia, Tian Laijin, Wang Hua
The Key Laboratory of Life-Organic Analysis and Key Laboratory of Pharmaceutical Intermediates and Analysis of Natural Medicine, School of Chemistry and Chemical Engineering, Qufu Normal University , Qufu 273165, Shandong, P. R. China.
J Org Chem. 2015 Nov 6;80(21):11073-9. doi: 10.1021/acs.joc.5b01637. Epub 2015 Oct 8.
A direct and straightforward approach for highly regioselective thiocyanation of imidazoheterocycles through sp(2) C-H functionalization has been realized at room temperature. Various C-3 thiocyanated imidazopyridines are formed in moderate to good yield. The present method exhibits a mild and selective access to a variety of imidazopyridine derivatives of pharmacological interest.
通过sp(2) C-H官能化对咪唑杂环进行高区域选择性硫氰化的直接且简便的方法已在室温下实现。各种C-3硫氰化的咪唑并吡啶以中等至良好的产率形成。本方法展示了一种温和且选择性地获得多种具有药理活性的咪唑并吡啶衍生物的途径。