1,3-Dipolar Cycloaddition of Imidazole Derivatives with Nitrile Oxide: Synthesis of Imidazo[1,2,4] oxadiazole Derivatives
1,3-Dipolar Cycloaddition of Imidazole Derivatives with Nitrile Oxide: Synthesis of Imidazo[1,2,4] oxadiazole Derivatives
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咪唑衍生物与氧化腈的1,3-偶极环加成反应：咪唑并[1,2,4]恶二唑衍生物的合成
DOI：
10.1002/ajoc.201700347
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发表时间：
2017-11-01
影响因子：
2.7
通讯作者：
Lin, Jun
中科院分区：
文献类型：
--
作者：
Jiang, Kun-Ming;Zhang, Jian-Qiang;Lin, Jun
通过2-氯-1H-苯并[d]咪唑与氧化腈的[3+2]环加成反应，合成了咪唑并[1，2，4]恶二唑衍生物。该策略可以方便地构建含有多种官能团的三环咪唑杂环衍生物。化合物3 p对KYSE 410细胞系显示出优异的细胞毒活性（IC 50 = 0.26 μ m）。这些三环咪唑杂环衍生物是有希望的药物发现的候选者。
A concise and efficient synthesis of imidazo[1,2,4] oxadiazole derivatives that proceeds through the [3+2] cycloaddition of 2-chloro-1H-benzo[d] imidazole with nitrile oxides has been developed. This strategy can conveniently construct tricyclic imidazole heterocyclic derivatives that contain a broad range of functional groups. Compound 3p showed excellent cytotoxic activity against the KYSE410 cell line (IC50 = 0.26 mu m). These tricyclic imidazole heterocyclic derivatives are promising candidates for drug discovery.