A simplified protocol for the automated production of 2‐[18F]fluoro‐3‐[2‐((S)‐3‐pyrrolinyl)methoxy]pyridine ([18F]nifene) on an IBA Synthera® module
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Published:2023-11-05
Issue:1
Volume:67
Page:31-36
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ISSN:0362-4803
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Container-title:Journal of Labelled Compounds and Radiopharmaceuticals
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language:en
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Short-container-title:Labelled Comp Radiopharmac
Author:
Bhuiyan Mohammed1ORCID,
Souris Jeffrey1,
Kucharski Anna12,
Freifelder Richard1,
Mukherjee Jogeshwar3,
Chen Chin‐Tu1
Affiliation:
1. Department of Radiology University of Chicago Chicago Illinois USA
2. Fermi National Accelerator Laboratory Batavia Illinois USA
3. Department of Radiological Science University of California, Irvine Irvine California USA
Abstract
The α4β2 nicotinic acetylcholine receptor (nAChR) ligand 2‐[18F]fluoro‐3‐[2‐((S)‐3‐pyrrolinyl)methoxy]pyridine ([18F]nifene) has been synthesized in 10% decay‐corrected radiochemical yield using the IBA Synthera® platform (IBA Cyclotron Solutions, Louvain‐la‐Neuve, Belgium) with an integrated fluidic processor (IFP). Boc‐nitronifene served as the precursor, and 20% trifluoroacetic acid (TFA) was used to deprotect the Boc‐group after radiolabeling. By omitting the solvent extraction step after radiolabeling, the process was simplified to a single step with no manual intervention. [18F]Nifene was obtained in decay‐corrected radiochemical yields of 10 ± 2% (n = 20) and radiochemical purity >99%. Typical specific radioactivities of 2700–4865 mCi/μmole (100–180 GBq/μmol) were measured at the end of synthesis; total synthesis times were about 1 h 40 min.
Funder
Center for Information Technology
Subject
Organic Chemistry,Spectroscopy,Drug Discovery,Radiology, Nuclear Medicine and imaging,Biochemistry,Analytical Chemistry