One-Step Synthesis of N-Succinimidyl-4-[18F]Fluorobenzoate ([18F]SFB)

Ida Nymann Petersen, Jacob Madsen, Christian Bernard Matthijs Poulie, Andreas Kjær, Matthias Manfred Herth


Herein, we present a one-step labeling procedure of N-succinimidyl-4-[18F]-fluorobenzoate ([18F]SFB) starting from spirocyclic iodonium ylide precursors. Precursor syntheses succeeded via a simple one-pot, two-step synthesis sequence, in yields of approximately 25%. Subsequent 18F-nucleophilic aromatic labeling was performed, and radiochemical incorporations (RCCs) from 5-35% were observed. Purification could be carried out using HPLC and subsequent solid phase extraction. Radiochemical purity (RCP) of >95% was determined. The total synthesis time, including purification and formulation, was no longer than 60 min. In comparison to the established 3-step synthesis route of [18F]SFB, this one-step approach avoids formation of volatile radioactive side-products and simplifies automatization.

TidsskriftBlood Cells, Molecules, and Diseases
Udgave nummer19
StatusUdgivet - 22 sep. 2019


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