Zhao Yingying, Hu Yancheng, Li Xincheng, Wan Boshun
Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 457 Zhongshan Road, Dalian 116023, China.
Org Biomol Chem. 2017 Apr 18;15(16):3413-3417. doi: 10.1039/c7ob00701a.
Oxadiazolones are first employed as the three-atom coupling partners in the TfNH-catalyzed cycloaddition with ynamides. This formal [3 + 2] cycloaddition allows a rapid synthesis of aminoimidazoles with a broad substrate scope. The approach also features a metal-free catalytic cycloaddition process, which may find applications in the synthesis of bioactive molecules. Besides, the resulting N-methyl products can further be readily converted to free N-H aminoimidazoles.
恶二唑酮首先被用作与炔酰胺进行三氟甲磺酰胺催化环加成反应中的三原子偶联伙伴。这种形式上的[3 + 2]环加成反应能够快速合成具有广泛底物范围的氨基咪唑。该方法还具有无金属催化环加成过程的特点，这可能在生物活性分子的合成中得到应用。此外，所得的N - 甲基产物可以很容易地进一步转化为游离的N - H氨基咪唑。
