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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Abstract

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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Authors

  • R. Koudih

  • A. Kostikov

  • M. Kovacevic

  • D. Jolly

  • V. Bernard-Gauthier

  • J. Chin

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