Вид документа : Статья из журнала Шифр издания : Автор(ы) : Shchegolkov E. V., Burgart Y. V., Matsneva D. A., Saloutin V. I., Borisevich S., Kadyrova R. A., Orshanskaya I. R., Zarubaev V. V. Заглавие : Polyfluoroalkylated antipyrines in Pd-catalyzed transformations Место публикации : RSC Advances. - 2021. - Vol. 11, № 56. - С. 35174-35181 Предметные рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: In the direct C–H arylation with arylhalogenides in the presence of Pd(OAc)2, trifluoromethyl-containing antipyrine reacts very slowly and incompletely owing to the low nucleophilicity of its C4 center. However, it was effective in modifying polyfluoroalkyl-substituted 4-bromo- and 4-iodo antipyrines by the Suzuki and Sonogashira reactions. It was established that using Pd2(dba)3 as catalyst and XPhos as phosphine ligand was the optimal catalytic system for the synthesis of 4-aryl- and 4-phenylethynyl-3-polyfluoroalkyl-antipyrines. Moreover, iodo-derivatives as the initial reagents were found to be more advantageous compared to bromo-containing analogs. It was found that 4-phenylethynyl-5-CF3-antipyrine has a moderate activity against the influenza virus A/Puerto Rico/8/34 (H1N1) and 4-iodo-5-CF3-antipyrine reveals a weak activity against the vaccine virus (strain Copenhagen) and bovine diarrhea virus (strain VC-1). Доп.точки доступа: Shchegolkov, E. V.; Burgart, Y. V.; Бургарт Янина Валерьевна; Matsneva, D. A.; Saloutin, V. I.; Borisevich, S.; Kadyrova, R. A.; Orshanskaya, I. R.; Zarubaev, V. V.