Білдинг-блоки на основі тетрагідропенталену, інспіровані природою: масштабований синтез для потреб медичної хімії

• Дата: 2023
• Автори: Smyrnov, Oleh K., Pashenko, Olexandr Ye.
• Формат: Стаття
• Мова: English
• Опубліковано: National University of Pharmacy 2023
• Теми: tetrahydropentalene; building blocks; medicinal chemistry; multigram synthesis; тетрагідропентален; білдинг-блоки; медична хімія; багатограмовий синтез
• Онлайн доступ: https://ophcj.nuph.edu.ua/article/view/299612
• Назва журналу: Journal of Organic and Pharmaceutical Chemistry

Inspired by the bioactivity of natural compounds with a bicyclo[3.3.0]octane core, the study focuses on developing tetrahydropentalene-2,5-dione (2,5-THP-dione) derivatives as potential building blocks for the use in medicinal chemistry. Using the commercially available 2,5-THP-dione, a number of alkylated derivatives and a monofunctional ketone were synthesized. Using optimized protocols for synthesis, target compounds were obtained with high yields on a multigram scale. These compounds are promising derivatives for further chemical derivatization and therapeutic use, and thus highlight the value of 2,5-THP-dione in creating complex molecular structures for drug discovery, as well as the importance of tetrahydropentalene derivatives as valuable building blocks in synthetic chemistry.