Pascali Giancarlo, Matesic Lidia, Zhang Bo, King Andrew T, Robinson Andrea J, Ung Alison T, Fraser Benjamin H
1Australian Nuclear Science and Technology Organisation, New South Wales, Australia.
2Brain and Mind Centre, University of Sydney, New South Wales, Australia.
EJNMMI Radiopharm Chem. 2017;2(1):9. doi: 10.1186/s41181-017-0028-6. Epub 2017 Jul 17.
The importance of the sulfur-fluorine bond is starting to increase in modern medicinal chemistry literature. This is due to a better understanding of the stability and reactivity of this moiety depending on the various oxidation states of sulfur. Furthermore, several commercial reagents used for mild and selective fluorination of organic molecules are based on the known reactivity of S-F groups. In this review, we will show how these examples are translating into the F field, both for use as stable tags in finished radiopharmaceuticals and as mildly reactive fluoride-relay intermediates. Finally, we also discuss current opportunities where examples of non-radioactive S-F applications/chemistry may be translated into future F radiochemistry applications.
在现代药物化学文献中,硫-氟键的重要性正开始提升。这是由于对该部分基于硫的各种氧化态的稳定性和反应活性有了更好的理解。此外,几种用于有机分子温和且选择性氟化的商业试剂是基于已知的S-F基团反应活性。在本综述中,我们将展示这些实例如何转化到氟领域,既用作成品放射性药物中的稳定标记,也用作温和反应性的氟中继中间体。最后,我们还讨论了当前的机会,即非放射性S-F应用/化学实例可转化为未来的氟放射化学应用。