1. Automated synthesis of [ 89 Zr]ZrCl 4 , [ 89 Zr]ZrDFOSquaramide-bisPh(PSMA) and [ 89 Zr]ZrDFOSquaramide-TATE.
- Author
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Noor A, Roselt PD, McGowan ER, Poniger S, Wheatcroft MP, and Donnelly PS
- Abstract
Background: Automated [
89 Zr]Zr-radiolabeling processes have the potential to streamline the production of [89 Zr]Zr-labelled PET imaging agents. Most radiolabeling protocols use [89 Zr][Zr(ox)4 ]4- as the starting material and oxalate is removed after radiolabeling. In some instances, radiolabeling with [89 Zr]ZrCl4 as starting material gives better radiochemical yields at lower reaction temperatures. In this work, a fully-automated process for production of [89 Zr]ZrCl4 is reported and its use for the synthesis of [89 Zr]ZrDFOSq-bisPhPSMA and [89 Zr]ZrDFOSq-TATE., Results: A simple automated process for the isolation of [89 Zr]ZrCl4 by trapping [89 Zr][Zr(ox)4 ]4- on a bicarbonate-activated strong anion exchange cartridge followed by elution with 0.1 M HCl in 1 M NaCl was developed. [89 Zr]ZrCl4 was routinely recovered from [89 Zr][Zr(ox)4 ]4- in > 95% yield in mildly acidic solution of 0.1 M HCl in 1 M NaCl using a fully-automated process. The [89 Zr]ZrCl4 was neutralized with sodium acetate buffer (0.25 M) removing the requirement for cumbersome manual neutralization with strong base. The mixture of [89 Zr]ZrCl4 was used for direct automated radiolabeling reactions to produce [89 Zr]Zr-DFOSquaramide-bisPhPSMA and [89 Zr]ZrDFOSquaramide-TATE in 80-90% over all RCY in > 95% RCP., Conclusions: This method for the production of [89 Zr]ZrCl4 does not require removal of HCl by evaporation making this process relatively fast and efficient. The fully automated procedures for the production of [89 Zr]ZrCl4 and its use in radiolabeling are well suited to support the centralized and standardized manufacture of multiple dose preparations of zirconium-89 based radiopharmaceuticals., (© 2024. The Author(s).)- Published
- 2024
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