Wang Huan, Huang Yao, Wu Qiaoyan, Lu Jun, Xu Yan-Li, Chen Yan-Yan
Guangxi Engineering Research Center for Pharmaceutical Molecular Screening and Druggability Evaluation, College of Pharmacy, Guangxi Key Laboratory of Diabetic Systems Medicine, Guilin Medical University, Guilin 541004, People's Republic of China.
J Org Chem. 2022 Oct 7;87(19):13288-13299. doi: 10.1021/acs.joc.2c01938. Epub 2022 Sep 27.
A visible-light-promoted difluoromethylation/cyclization of 2-vinyloxy arylalkynes was developed, providing a variety of bis(difluoromethyl)-substituted benzofurans in moderate to good yields. A plausible mechanism involving difluoromethyl radical cascade cyclization and solvent-promoted ionic addition was proposed. This protocol has the advantages of having mild reaction conditions, simple operation, and good functional group tolerance.
开发了一种可见光促进的2-乙烯氧基芳基炔烃的二氟甲基化/环化反应,以中等至良好的产率提供了多种双(二氟甲基)取代的苯并呋喃。提出了一种合理的机理,涉及二氟甲基自由基级联环化和溶剂促进的离子加成。该方法具有反应条件温和、操作简单、官能团耐受性好等优点。