[18F]Fluoroaliphatic carboxylic acids are important PET tracers that have demonstrated a considerable potential to address the fatty acid oxidation-dependent processes in clinical patients. Herein, we report an efficient radiosynthetic approach to ω-[18F]fluoroaliphatic carboxylic esters and acids by nucleophilic radiofluorination of the readily available iodocarboxylic esters. Methyl 6-[18F]fluorohexanoate was further applied as a starting material for the preparation of the succinimide ester (NHS ester)-containing bifunctional radiofluorinated prosthetic group in two simple steps, 10 min each. The synthesized NHS ester of 6-[18F]fluorohexanoic acid can serve as an important reagent for a quick and efficient conjugation with peptides or proteins via amino groups of lysines.
Bibliographical noteFunding Information:
This work was supported by a research grant from the Russian Science Foundation (RSF‐16‐13‐10081‐P) and the Ministry of Science and Higher Education of the Russian Federation (grant 075‐15‐2019‐1925). The research was carried out using the core facilities of TPU's “Physical and chemical methods of analysis”.
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- Fluorinated compounds
- PET radiotracers
- Synthetic methods