Closing the gap between (19)F and (18)F chemistry.
Closing the gap between (19)F and (18)F chemistry.
复制标题
缩小（19）F和（18）F化学之间的差距。
DOI：
10.1186/s41181-021-00143-y
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发表时间：
2021-09-25
影响因子：
4.6
通讯作者：
Gouverneur V
中科院分区：
文献类型：
--
作者：
Ajenjo J;Destro G;Cornelissen B;Gouverneur V
正电子发射断层扫描（PET）已成为药物发现和诊断的宝贵工具。直接影响医学多年。在过去的二十年中，有18F的前体的多样性，18F-RadioChemistion以快速的速度进行了进步不需要这些进步的关键是包括新的激活模式以促进18F的企业。在过渡金属催化，光电毒素催化和有机催化中的19F氟化以及新型18F标记的氟化试剂的可用性使得能够在复合物（BIO）分子上进行18F的新过程。关注C – 18F债券形成的方法。对19F化学的影响，许多实验室都将他们的努力重新集中在使用核氟代替分子氟气体的氟化试剂的发展上。
Positron emission tomography (PET) has become an invaluable tool for drug discovery and diagnosis. The positron-emitting radionuclide fluorine-18 is frequently used in PET radiopharmaceuticals due to its advantageous characteristics; hence, methods streamlining access to 18F-labelled radiotracers can make a direct impact in medicine. For many years, access to 18F-labelled radiotracers was limited by the paucity of methodologies available, and the poor diversity of precursors amenable to 18F-incorporation. During the last two decades, 18F-radiochemistry has progressed at a fast pace with the appearance of numerous methodologies for late-stage 18F-incorporation onto complex molecules from a range of readily available precursors including those that do not require pre-functionalisation. Key to these advances is the inclusion of new activation modes to facilitate 18F-incorporation. Specifically, new advances in late-stage 19F-fluorination under transition metal catalysis, photoredox catalysis, and organocatalysis combined with the availability of novel 18F-labelled fluorination reagents have enabled the invention of novel processes for 18F-incorporation onto complex (bio)molecules. This review describes these major breakthroughs with a focus on methodologies for C–18F bond formation. This reinvigorated interest in 18F-radiochemistry that we have witnessed in recent years has made a direct impact on 19F-chemistry with many laboratories refocusing their efforts on the development of methods using nucleophilic fluoride instead of fluorination reagents derived from molecular fluorine gas.
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影响因子：
8.4
作者：
Benedetto, Elena;Tredwell, Matthew;Gouverneur, Veronique
通讯作者：
Gouverneur, Veronique
影响因子：
2.7
作者：
Andres, Miriam;Buil, Maria Antonia;Roberts, Richard S.
通讯作者：
Roberts, Richard S.
影响因子：
1.9
作者：
ARGENTINI, M;WIESE, C;WEINREICH, R
通讯作者：
WEINREICH, R
影响因子：
3.1
作者：
Bishop, A;Satyamurthy, N;Barrio, JR
通讯作者：
Barrio, JR
影响因子：
1.8
作者：
Cardinale, Jens;Ermert, Johannes;Coenen, Heinz H.
通讯作者：
Coenen, Heinz H.