文献类型：期刊文献

英文题名：Synthesis of gem-Difluorinated 2,3-Dihydrobenzofurans Using Freon-22 via [4+1] Annulation of Difluorocarbene and Antitumor Activity Evaluation

作者：Zhou, Qianying Huang, Mi Shen, Yongcun Chen, Zhenling Xu, Liying Yang, Zhigang

第一作者：Zhou, Qianying

通信作者：Yang, ZG[1];Chen, ZL[2]

机构：[1]Wuhan Univ Technol, Sch Chem Chem Engn & Life Sci, Wuhan 430070, Peoples R China;[2]Wuhan Univ, Zhongnan Hosp, Sch Pharmaceut Sci, Dept Radiol, Wuhan 430071, Peoples R China;[3]Lund Univ, Clin Res Ctr, Dept Clin Sci, S-21428 Malmo, Sweden;[4]Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China

第一机构：Wuhan Univ Technol, Sch Chem Chem Engn & Life Sci, Wuhan 430070, Peoples R China

通信机构：corresponding author), Wuhan Univ, Zhongnan Hosp, Sch Pharmaceut Sci, Dept Radiol, Wuhan 430071, Peoples R China;corresponding author), Guizhou Inst Technol, Sch Chem Engn, Guiyang 550003, Peoples R China.|贵州理工学院化学工程学院;贵州理工学院;

年份：2024

卷号：26

期号：6

起止页码：1212-1217

外文期刊名：ORGANIC LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001160867600001)，CCR-EXPANDED(收录号:WOS:001160867600001)】；

基金：We are thankful for financial support from the National Key Research and Development Program of China (Grant No. 2018YFA0704000), the Natural Science Foundation of Hubei Province (2022CFB204), and the Academic New Seedling Plan Project of Guizhou Institute of Technology (GZLGXM-18).

语种：英文

摘要：As an inexpensive industrial chemical, chlorodifluoromethane (Freon-22), despite its relatively low reactivity, can serve as a practical CF2 source for the construction of gem-difluorinated ring structures. Here, we develop a protocol for the efficient assembly of valuable fluorinated 2,3-dihydrobenzofurans from the [4 + 1] annulation in good yields under basic conditions. The reliable practicability and scalability of the process have also been demonstrated by preparation at the multigram scale, late-stage modifications of pharmaceutical molecules, and potential antitumor potency.