Синтез різноманітних піридинів, анельованих функціоналізованими шестичленними насиченими циклами, для досліджень у галузі медичної хімії

• Дата: 2023
• Автори: Yehorov, Dmytro V., Subota, Andrii I.
• Формат: Стаття
• Мова: English
• Опубліковано: National University of Pharmacy 2023
• Теми: organic synthesis; heterocyclic compounds; pyridines; building blocks; organofluorines; “magic methyl”; scaffold hopping; органічний синтез; гетероциклічні сполуки; піридини; фторорганічні сполуки; «чарівний метил»; скафолдне прогнозування
• Онлайн доступ: https://ophcj.nuph.edu.ua/article/view/289263
• Назва журналу: Journal of Organic and Pharmaceutical Chemistry

The article describes a set of pyridines annulated with functionalized 6-membered saturated rings, which are attractive building blocks for the synthesis of diversified compound libraries in medical chemistry. A certain array of compounds includes pyridines with condensed cyclohexane, piperidine and tetrahydropyran cycles containing keto-, amino-, carboxylic groups, as well as fluorinated fragments. The synthesis of the compounds using the procedure previously developed by us via CuCl2-catalyzed condensation of propargylamine with ketones was performed. The limits of application of this reaction were further expanded and determined in this work compared to our previous results. Condensed pyridines, which proved problematic or impossible to obtain by this method, were synthesized using other synthetic pathways. Thus, the study offers a number of new building blocks for use in drug discovery.