School of Chemistry and Chemical Engineering, Hefei University of Technology, 193 Tunxi Road, Anhui 230000, People's Republic of China.
School of Food and Biological Engineering, Hefei University of Technology, 193 Tunxi Road, Anhui 230009, China.
J Org Chem. 2020 Jul 2;85(13):8723-8731. doi: 10.1021/acs.joc.0c00894. Epub 2020 Jun 22.
The incorporation of a perfluoroalkyl group (R) into drug candidates has become an increasingly important strategy in drug molecule design. In this study, the silver-mediated perfluoroalkylation reaction based on the addition-elimination process of terminal alkynes which was initiated by a perfluoroalkyl radical to form a C(sp)-R bond has been developed. The reaction proceeds under mild conditions using readily available, low-cost perfluoroalkyl iodides as the sources of the R group. This method allows access to a variety of perfluoroalkylated alkynes.
将全氟烷基（R）引入候选药物中已成为药物分子设计中越来越重要的策略。在本研究中，开发了基于银介导的全氟烷基化反应，该反应基于末端炔烃的加成-消除过程，由全氟烷基自由基引发，形成 C(sp)-R 键。该反应在温和条件下进行，使用易得、低成本的全氟碘代烷作为 R 基团的来源。该方法可用于合成各种全氟烷基化的炔烃。
