A Fluorine-18 Radiolabeling Method Enabled by Rhenium(I) Complexation Circumvents the Requirement of Anhydrous Conditions

作者：Klenner, Mitchell A.; Pascali, Giancarlo^*; Zhang, Bo; Sia, Tiffany R.; Spare, Lawson K.; Krause-Heuer, Anwen M.; Aldrich-Wright, Janice R.; Greguric, Ivan; Guastella, Adam J.; Massi, Massimiliano; Fraser, Benjamin H.^*

来源：Chemistry - A European Journal, 2017, 23(27): 6499-6503.

DOI：10.1002/chem.201700440

• fluorine-18 radiolabeling
• late-stage fluorination
• microfluidics
• pet chemistry
• rhenium complexes

Azeotropic distillation is typically required to achieve fluorine-18 radiolabeling during the production of positron emission tomography (PET) imaging agents. However, this time-consuming process also limits fluorine-18 incorporation, due to radioactive decay of the isotope and its adsorption to the drying vessel. In addressing these limitations, the fluorine-18 radiolabeling of one model rhenium(I) complex is reported here, which is significantly improved under conditions that do not require azeotropic drying. This work could open a route towards the investigation of a simplified metal-mediated late-stage radiofluorination method, which would expand upon the accessibility of new PET and PET-optical probes.

• 出版日期2017-5-11