Buckingham Faye, Gouverneur Véronique
University of Oxford , Chemistry Research Laboratory , 12 Mansfield Road , OX1 3UQ , Oxford , UK . Email:
Chem Sci. 2016 Mar 1;7(3):1645-1652. doi: 10.1039/c5sc04229a. Epub 2015 Dec 17.
Positron emission tomography (PET) is becoming more frequently used by medicinal chemists to facilitate the selection of the most promising lead compounds for further evaluation. For PET, this entails the preparation of C- or F-labeled drugs or radioligands. With the importance of chirality and fluorine substitution in drug development, chemists can be faced with the challenge of preparing enantiopure molecules featuring the F-tag on a stereogenic carbon. Asymmetric F-fluorination is an emerging field of research that provides an alternative to resolution or conventional S2-based radiochemistry. To date, both transition metal complexes and organomediators have been successfully employed for F-incorporation at a stereogenic carbon.
正电子发射断层扫描（PET）在药物化学领域的应用越来越频繁，有助于筛选出最有潜力的先导化合物进行进一步评估。对于PET而言，这需要制备碳或氟标记的药物或放射性配体。鉴于手性和氟取代在药物开发中的重要性，化学家可能会面临制备在立体碳上带有氟标签的对映体纯分子的挑战。不对称氟氟化是一个新兴的研究领域，为拆分或传统的基于S2的放射化学提供了一种替代方法。迄今为止，过渡金属配合物和有机媒介物都已成功用于在立体碳上引入氟。
