One-step synthesis of N-succinimidyl-4-[18F]Fluorobenzoate ([18F]SFB)
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- OA-One-Step Synthesis
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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.
Originalsprog | Engelsk |
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Artikelnummer | 3436 |
Tidsskrift | Molecules |
Vol/bind | 24 |
Udgave nummer | 19 |
Antal sider | 7 |
ISSN | 1431-5157 |
DOI | |
Status | Udgivet - 22 sep. 2019 |
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