Abstract
A simple and rapid method for 18F radiolabelling of [GaF3(BnMe2‐tacn)] by 18F/19F isotopic exchange is described. The use of MeCN/H2O or EtOH/H2O (75:25) and aqueous [18F]F− (up to 200 MBq) with heating (80 °C, 10 min) gave 66±4 % 18F incorporation at a concentration of 268 nm, and 37±5 % 18F incorporation at even lower concentration (27 nm), without the need for a Lewis acid promoter. A solid‐phase extraction method was established to give [Ga18F19F2(BnMe2‐tacn)] in 99 % radiochemical purity in an EtOH/H2O mixture.
Highlights
A simple and rapid method for 18F radiolabelling of [GaF3(BnMe2-tacn)] by 18F/19F isotopic exchange is described
The 18F half-life is sufficient to allow for a certain degree of manipulation of the synthesis, provided that the radiolabelling occurs in the later stages of the synthesis
The most commonly used positron emission tomography (PET) radiotracers are organic molecules where the radioactive fluorine atom is attached to a carbon atom
Summary
A simple and rapid method for 18F radiolabelling of [GaF3(BnMe2-tacn)] by 18F/19F isotopic exchange is described. Work on the “Al-F” system developed by McBride and co-workers demonstrated that radiofluorination can be achieved by heating AlCl3, [18F]FÀ, and a pentadentate NOTAderived ligand together in aqueous solution at pH 3.9–4.2 and 100 8C (NOTA = 1,4,7-triazacyclononane-1,4,7-triacetic acid).[14] This was an important breakthrough, providing the first example of a metal chelate system for [18F]FÀ capture in water, and exploiting coordination chemistry to determine fluoride incorporation.
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