Journal of Fluorine Chemistry ( IF 1.9 ) Pub Date : 2024-01-06 , DOI: 10.1016/j.jfluchem.2024.110240 Larisa Gurskaya , Larisa Politanskaya , Jiaying Wang , Polina Ilyina , Alexandrina Volobueva , Vladimir Zarubaev
A convenient and efficient method for the synthesis of fluorinated phenanthridin-6(5H)-ones from the corresponding 2-isocyanato-1,1′-biphenyls mediated by trifluoromethanesulfonic acid in chlorobenzene is described. The reaction uses readily available starting materials, takes place under very mild reaction conditions (r. t.) and provides access to biologically promising fluorinated heterocycles in good to excellent yields. Synthesized compounds were tested in vitro for cytotoxicity in MDCK cell line and for antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1).
中文翻译:
新型氟化菲啶-6(5H)-酮衍生物的高效合成及其体外抗病毒活性评价
描述了一种在氯苯中以三氟甲磺酸为介导的从相应的2-异氰酸基-1,1'-联苯合成氟化菲啶-6(5 H )-酮的简便有效的方法。该反应使用容易获得的起始原料,在非常温和的反应条件(rt)下进行,并以良好至优异的收率获得具有生物学前景的氟化杂环。在体外测试了合成化合物在 MDCK 细胞系中的细胞毒性以及针对流感病毒 A/Puerto Rico/8/34 (H1N1) 的抗病毒活性。