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

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 al...

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Bibliographic Details
Date:2023
Main Authors: Smyrnov, Oleh K., Pashenko, Olexandr Ye.
Format: Article
Language:English
Published: National University of Pharmacy 2023
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Online Access:https://ophcj.nuph.edu.ua/article/view/299612
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Journal Title:Journal of Organic and Pharmaceutical Chemistry

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Journal of Organic and Pharmaceutical Chemistry
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Summary: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.