Results
Title

Method for indirect radiofluorination with [<sup>18</sup>F]FDG by biorthogonal reaction.

Authors

Simeonova, Gergana; Todorov, Boyan; Lyubomirova, Valentina

Abstract

The [18F]-fluorodeoxyglucose ([18F]FDG) is a universal PET—radiopharmaceutical routinely applauded (oncology, cardiology and neurology) and produced by medical cyclotrons (18O(p,n)18F) in many clinics of Nuclear Medicine. Current trend in medicine is to become more personalized and new types of therapeutic and diagnostic radiopharmaceuticals are applied involving pre-targeting strategy. Using existing facilities and equipment in clinics for specific modification of approved radiopharmaceutical as [18F]FDG will provide unique toolbox in hands of physicians and will forward personalization of therapy in Nuclear Medicine. In the present study investigation over conjugation between [18F]FDG and aminooxy functionalized tetrazine by chemoselective oxime bond formation was done. Method for direct labeling of tetrazine derivative (clickable with trans cyclooctene moieties) with [18F]FDG used standard clinical laboratory settings was developed. The synthesis was carried out in a weakly acidic condition—pH 4–4.3; at 70 °C and in the presence of p-methoxyaniline as a catalyst. The progress of the reactions was monitored by radio-TLC, HPLC and to conform final formulation IR-ATR spectroscopy was used.

Publication

European Physical Journal: Special Topics, 2023, Vol 232, Issue 10, p1555

ISSN

1951-6355

Publication type

Academic Journal

DOI

10.1140/epjs/s11734-023-00885-7