氟化构建块

我们将通过丰富的含氟构建模块组合确保您的工作持续推进,其中包含具有常见且理想取代基的化合物,例如三氟甲基(TFM)、二氟甲基(DFM)、三氟甲磺酸酯及五氟硫基。 在有机分子中引入氟原子或氟代烷基,可在最小立体位阻干扰下调节其物理化学性质(如稳定性、反应性、亲脂性及酸度),并能显著提升先导化合物的筛选效率。¹ 此外,相较于非氟化同系物,氟化构建模块展现出更优异的热稳定性。 据估计,约 30% 的所有新批准药物2、超过 50% 的批准畅销药3(如立普妥® 和百忧解®)以及约 25% 的许可除草剂1(如三氟草胺和氟萘胺)都含有一个或多个氟原子,这些产品的年销售额高达数十亿美元。
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- Article: AlPhos and [(AlPhosPd)2•COD] for Pd-Catalyzed Fluorination
Fluorine containing aromatics (ArF) are desirable compounds with applications in medicinal chemistry and the agricultural industry.
参考文献
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Fujiwara T, O'Hagan D. 2014. Successful fluorine-containing herbicide agrochemicals. Journal of Fluorine Chemistry. 16716-29. https://doi.org/10.1016/j.jfluchem.2014.06.014
2.
Zhou Y, Wang J, Gu Z, Wang S, Zhu W, Aceña JL, Soloshonok VA, Izawa K, Liu H. 2016. Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II?III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas. Chem. Rev.. 116(2):422-518. https://doi.org/10.1021/acs.chemrev.5b00392
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Han J, Butler G, Moriwaki H, Konno H, Soloshonok VA, Kitamura T. Kitamura Electrophilic Fluorination Using HF as a Source of Fluorine. Molecules. 25(9):2116. https://doi.org/10.3390/molecules25092116
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