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

Molecules

Jacob Madsen¹  Christian Bernard Matthijs Poulie²  Matthias Manfred Herth³  Ida Nymann Petersen³  Andreas Kjær⁴ 

[1] PET, University Hospital (Rigshospitalet), Blegdamsvej 9, DK-2100 Copenhagen, Denmark;Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 9, DK-2100 Copenhagen, Denmark;;Department of Clinical Physiology, Nuclear Medicine &Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Jagtvej 160, DK-2100 Copenhagen, Denmark;

关键词: N-succinimidyl-4-[¹⁸F]fluorobenzoate;    [¹⁸F]SFB;    iodonium ylides;    fluorine-18;    PET;   

DOI  :  10.3390/molecules24193436

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown