Automated radiosynthesis of N-succinimidyl 3-(di-tert-butyl[18F]fluorosilyl)benzoate ([18F]SiFB) for peptides and proteins radiolabeling for positron emission tomography

  • Koudih R
  • Kostikov A
  • Kovacevic M
 et al. 
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Recently, silicon fluoride building blocks (SiFA) have emerged as valuable and promising tools to overcome challenges in the labeling of peptides and proteins for positron emission tomography (PET). Herein, we report a fully automated synthesis of N-succinimidyl 3-(di-tert-butyl[18F]fluorosilyl)benzoate ([18F]SiFB) by a commercially available Scintomics Hot Box 3 synthesis module, to be used as a prosthetic group for peptide and protein labeling. The drying of K2.2.2./K18F complex was performed according to the Munich method modified by our group (avoiding azeotropic drying) using oxalic acid to neutralize the base from the18F-containing QMA eluent. This K2.2.2./K18F complex was then used for SiFA18F-19F isotopic exchange followed by a fast purification by a solid-phase-extraction (SPE) to afford [18F]SiFB with an average preparative radiochemical yield (RCY) of 24±1% (non-decay corrected (NDC)) within a synthesis time of 30min. The [18F]SiFB produced by automated synthesis was then used for the18F-labeling of rat serum albumin (RSA) as a proof of applicability. © 2014 Elsevier Ltd.

Author-supplied keywords

  • Automated synthesis
  • Biomolecules labeling
  • Fluorine 18
  • PET imaging
  • SiFA
  • Silicon-fluoride building blocks

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  • R. Koudih

  • A. Kostikov

  • M. Kovacevic

  • D. Jolly

  • V. Bernard-Gauthier

  • J. Chin

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