Abstract
The 16α-[18F]Fluoroestradiol ([18F]FES) is an established PET radiotracer for estrogen positive (ER+) breast cancer. Although the radiosynthesis is well-described, the majority of the published methods suffer from modest or irreproducible yields and time-intensive purification procedures. In view of the considerable clinical applications, development of a more efficient and faster synthesis of [18F]FES still remains a task of a significant practical importance. [18F]FES was produced by a direct nucleophilic radiofluorination of 3-O-methoxymethyl-16,17-O-sulfuryl-16-epiestriol (MMSE), followed by acidic hydrolysis using HCl/CH3CN. [18F]Fluoride retained on a QMA carb cartridge (46 mg) was eluted by solution of 1.2 mg of tetrabutylammonium tosylate (TBAOTs) in EtOH. After fluorination reaction (0.3 mg MMSE, 1 ml of CH3CN/100 °C, 5 min) [18F]FES was isolated by single-cartridge SPE purification using OASIS WAX 3cc, elution accomplished with aqueous ethanol of different concentrations. On а GE TRACERlab FX N Pro automated module [18F]FES (formulated in normal saline with 5% EtOH) was obtained in 33 ± 3% yield (n = 5, non-decay corrected) within 32 min. Reduction of precursor amount, exclusion of azeotropic drying step and simplification of purification make the suggested method readily adaptable to various automated synthesizers and offers significant cost decrease.
Funding source: N.P. Bechtereva Institute of Human Brain, Russian Academy of Sciences
Author contribution: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
Research funding: This study was supported by state funding at the N.P. Bechtereva Institute of Human Brain, Russian Academy of Sciences.
Conflict of interest statement: The authors declare no conflicts of interest.
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