PEACE · Photocatalyzed enantiodivergent synthesis of homoallylic and carboxylic acids featuring heterodiaryl quaternary carbon stereocenters
„Хоризонт Европа“ — Действия „Мария Склодовска-Кюри“
- Период
- 2023-10-01 → 2025-09-30
- Финансиране от ЕС
- 165 313 €
- Участници
- 2
- Схема
- HORIZON-TMA-MSCA-PF-EF
Линиите свързват координатора с партньорите.
Накратко на български
Фотокатализата се използва за създаване на специфични въглеродни структури, като например хомоалилни и карбоксилни киселини. Това помага за намаляване на разходите и вредните емисии при производството на активни фармацевтични съставки.
Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.
Резултати накратко
Photocatalyzed enantiodivergent synthesis of homoallylic and carboxylic acids featuring heterodiaryl quaternary carbon stereocenters
The PEACE project sought to tackle novel research and innovation (R&I) methods for creating diaryl all-carbon quaternary carbon centers through a pioneering photocatalyzed enantiodivergent approach. By utilizing a single chiral catalytic system, the project aimed to significantly reduce the methodology's costs. This involved devising substrate-based enantiodivergent strategies, relying on carefully chosen reaction partners to revolutionize the synthesis of both enantiomers of stereocenters encompassing diaryl quaternary carbon centers. Specifically, the outcomes, results, and impacts of PEACE were expected to manifest in several dimensions: (a) Scientific Impact: PEACE aimed to expand knowledge in sustainable catalytic synthesis of all-carbon stereocenters, paving the way for new scientific approaches adaptable and scalable in both academic and industrial settings. This effort aimed to bolster investment in green R&I while educating researchers, both young and seasoned, on novel catalytic and sustainable processes. (b) Economic/Technological/Societal Impact: Furthermore, the project's outcomes aimed to address the pressing demand for a more sustainable future in high-value fine-chemical production. Designing innovative and economically sustainable approaches to quaternary stereocenters posed a significant challenge in the fine chemical industry. PEACE aimed to impact this sector by developing and designing a new divergent synthesis utilizing a single catalytic system, thus promoting a greener future. With a focus on medicinal chemistry, this project was poised to significantly decrease the overall synthesis costs of Active Pharmaceutical Ingredients (APIs).
Текст от CORDIS, на английски · Данни: CORDIS, © Европейски съюз
Цел на проекта
The synthesis of heterodiaryl-based quaternary stereocenters is a very challenging task in organic synthesis, especially in the creation of highly functional scaffolds. Tetrahedral, congested carbons centers bearing two different aryl moieties have great importance for structure−activity relationship (SAR) studies in pharmaceutical discovery programs. Their presence in biological active natural products makes them fundamental for the future development of new bioactive molecules. Up to now, their synthesis requires unsustainable methodologies that involve high cost, unfavourable step-economy and a negative waste profile features and need highly reactive compounds that only permit low functional groups tolerance. Moreover, the enantioselective synthesis of both product enantiomer requires the use of both catalyst enantiomers raising the cost of the process. Therefore, it is fundamental to develop a simple, scalable and environmentally friendly approach for the enantioselective synthesis of compounds comprising heterodiaryl-quaternary stereocenters and functionalized derivatives. The PEACE project aims to develop a novel photocatalyzed, enantiodivergent synthesis process leading to such heterodiarylated all-carbon stereocenters. The designed dual catalytic cycle of the PEACE project merges Pd and photoredox catalysis to promote the enantioselective construction of new sp3-sp2 carbon-carbon bonds resulting into products featuring a quaternary carbon stereocenter. The enantiodivergent strategy is based on a judicious choice of structurally modular reaction partners with switchable aryl groups. The combination of VCCs (vinyl,aryl-substituted cyclic carbonates) and a new aryl radical precursor offers an innovative enantiodivergent reaction pathway leading to challenging quaternary stereocenters creating impetus in the area of organic synthetic chemistry, and revolutionizing similar synthetic designs in the pharmaceutical industry.
Оригинален текст от CORDIS (на английски).
Участници
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Данни: CORDIS, © Европейски съюз