通过Togni试剂介导的三氟甲基化反应，随后经PhIO介导的氮杂环丙烷化反应合成三氟甲基化的2-氮杂环丙烷。
Synthesis of trifluoromethylated 2-azirines through Togni reagent-mediated trifluoromethylation followed by PhIO-mediated azirination.
作者信息
Sun Jiyun, Zhen Xiaohua, Ge Huaibin, Zhang Guangtao, An Xuechan, Du Yunfei
机构信息
Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300072, China.
出版信息
Beilstein J Org Chem. 2018 Jun 15;14:1452-1458. doi: 10.3762/bjoc.14.123. eCollection 2018.
The reaction of enamine compounds with the Togni reagent in the presence of CuI afforded β-trifluoromethylated enamine intermediates, which were converted directly to biologically interesting trifluoromethylated 2-azirines by an iodosobenzene (PhIO)-mediated intramolecular azirination in a one-pot process.
在碘化亚铜（CuI）存在下，烯胺化合物与托格尼试剂反应生成β-三氟甲基化烯胺中间体，这些中间体通过碘苯（PhIO）介导的分子内氮杂环丙烷化反应在一锅法中直接转化为具有生物学意义的三氟甲基化2-氮杂环丙烷。
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