» Articles » PMID: 25190038

Neither Azeotropic Drying, nor Base nor Other Additives: a Minimalist Approach to (18)F-labeling

Overview
Journal Org Biomol Chem
Specialties Biochemistry
Chemistry
Date 2014 Sep 6
PMID 25190038
Citations 37
Authors
Affiliations
Soon will be listed here.
Abstract

A novel, efficient, time-saving and reliable radiolabeling procedure via nucleophilic substitution with [(18)F]fluoride is described. Different radiolabeled aliphatic and aromatic compounds were prepared in high radiochemical yields simply by heating of quaternary anilinium, diaryliodonium and triarylsulfonium [(18)F]fluorides in suitable solvents. The latter were obtained via direct elution of (18)F(-) from an anion exchange resin with alcoholic solutions of onium precursors. Neither azeotropic evaporation of water, nor a base, nor any other additives like cryptands or crown ethers were necessary. Due to its simplicity this method should be highly suitable for automated radiosyntheses, especially in microfluidic devices.

Citing Articles

Fully Automated Production of ((()-1-Carboxy-5-(6-([F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic Acid ([F]JK-PSMA-7).

Krapf P, Wicher T, Zlatopolskiy B, Ermert J, Neumaier B Pharmaceuticals (Basel). 2025; 18(1).

PMID: 39861180 PMC: 11769433. DOI: 10.3390/ph18010119.


Simple and Efficient Synthesis of -Succinimidyl-4-[F]fluorobenzoate ([F]SFB)-An Important Intermediate for the Introduction of Fluorine-18 into Complex Bioactive Compounds.

Orlovskaya V, Fedorova O, Viktorov N, Krasikova R Pharmaceuticals (Basel). 2025; 17(12.

PMID: 39770565 PMC: 11677304. DOI: 10.3390/ph17121723.


Preclinical evaluation of an F-labeled N-acryloyllysine piperazide for covalent targeting of transglutaminase 2.

Wodtke R, Laube M, Hauser S, Meister S, Ludwig F, Fischer S EJNMMI Radiopharm Chem. 2024; 9(1):1.

PMID: 38165538 PMC: 10761660. DOI: 10.1186/s41181-023-00231-1.


Preparation of F-Labeled Tracers Targeting Fibroblast Activation Protein via Sulfur [F]Fluoride Exchange Reaction.

Craig A, Kogler J, Laube M, Ullrich M, Donat C, Wodtke R Pharmaceutics. 2023; 15(12).

PMID: 38140090 PMC: 10747913. DOI: 10.3390/pharmaceutics15122749.


Preparation of -Methyl-6-[F]fluoro- and 5-Hydroxy-7-[F]fluorotryptophans as Candidate PET-Tracers for Pathway-Specific Visualization of Tryptophan Metabolism.

Kolks N, Neumaier F, Neumaier B, Zlatopolskiy B Int J Mol Sci. 2023; 24(20).

PMID: 37894930 PMC: 10607147. DOI: 10.3390/ijms242015251.