Synthesis of 18F-labeled acyclic purine and pyrimidine nucleosides intended for monitoring gene expression


Synthesis of 18F-labeled acyclic purine and pyrimidine nucleosides intended for monitoring gene expression

Grote, M.; Noll, B.; Noll, S.

Non-invasive imaging of genes which are introduced into cells is a useful method for gene therapy monitoring. The labeling of acyclic purine and pyrimidine nucleoside derivatives with fluorine-18 required for the HSV-1 tk imaging approach with Positron Emission Tomography (PET) 18 is described. The methoxytritylated and tosylated precursors were radiolabeled using a K[18F]F/kryptofix 2.2.2TM complex, followed by removal of the protecting groups under acidic conditions and HPLC purification. The radiochemical yields of the 18F-tracers amount to 5 - 15 % (decay corrected) after a synthesis time of 85 - 95 min, the radiochemical purity was > 98 % with an average specific activity of 19 GBq/μmol at the end of synthesis.

Keywords: fluorine-18; PET; gene expression; HSV-1 tk

  • Radiochimica Acta 93(2005)9-10, 585-588

Permalink: https://www.hzdr.de/publications/Publ-7032
Publ.-Id: 7032