Applications of Fluorine in Medicinal Chemistry,Journal of Medicinal Chemistry

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Applications of Fluorine in Medicinal Chemistry
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2015-07-22 00:00:00 , DOI: 10.1021/acs.jmedchem.5b00258
Eric P. Gillis ₁ , Kyle J. Eastman ₁ , Matthew D. Hill ₁ , David J. Donnelly ₂ , Nicholas A. Meanwell ₁

Affiliation

The role of fluorine in drug design and development is expanding rapidly as we learn more about the unique properties associated with this unusual element and how to deploy it with greater sophistication. The judicious introduction of fluorine into a molecule can productively influence conformation, pK_a, intrinsic potency, membrane permeability, metabolic pathways, and pharmacokinetic properties. In addition, ¹⁸F has been established as a useful positron emitting isotope for use with in vivo imaging technology that potentially has extensive application in drug discovery and development, often limited only by convenient synthetic accessibility to labeled compounds. The wide ranging applications of fluorine in drug design are providing a strong stimulus for the development of new synthetic methodologies that allow more facile access to a wide range of fluorinated compounds. In this review, we provide an update on the effects of the strategic incorporation of fluorine in drug molecules and applications in positron emission tomography.

中文翻译：

氟在药物化学中的应用

随着我们更多地了解与这种不寻常元素相关的独特特性以及如何以更高的复杂度进行部署，氟在药物设计和开发中的作用正在迅速扩大。明智地将氟引入分子中可以有效地影响构象，p K _a，内在效能，膜通透性，代谢途径和药代动力学特性。另外¹⁸F已经被确定为与体内成像技术一起使用的有用的正电子发射同位素，其可能在药物发现和开发中具有广泛的应用，通常仅受标记化合物的方便合成可及性的限制。氟在药物设计中的广泛应用为开发新的合成方法提供了强大的动力，新的合成方法可更轻松地获得各种氟化化合物。在这篇综述中，我们提供了氟在药物分子中的战略性掺入及其在正电子发射断层扫描中的应用的最新进展。

更新日期：2015-07-22

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