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

被引:1
|
作者
Bhuiyan, Mohammed [1 ,4 ]
Souris, Jeffrey [1 ]
Kucharski, Anna [1 ,2 ]
Freifelder, Richard [1 ]
Mukherjee, Jogeshwar [3 ]
Chen, Chin-Tu [1 ,4 ]
机构
[1] Univ Chicago, Dept Radiol, Chicago, IL USA
[2] Fermilab Natl Accelerator Lab, Batavia, IL USA
[3] Univ Calif Irvine, Dept Radiol Sci, Irvine, CA USA
[4] Univ Chicago, Dept Radiol, Chicago, IL 60637 USA
关键词
IBA Synthera (R); radiosynthesis; alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR) ligand; F-18]nifene; NICOTINIC ACETYLCHOLINE-RECEPTORS; PET; F-18-NIFENE; BINDING;
D O I
10.1002/jlcr.4071
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR) ligand 2-[F-18]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([F-18]nifene) has been synthesized in 10% decay-corrected radiochemical yield using the IBA Synthera (R) 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. [F-18]Nifene was obtained in decay-corrected radiochemical yields of 10 +/- 2% (n = 20) and radiochemical purity >99%. Typical specific radioactivities of 2700-4865 mCi/mu mole (100-180 GBq/mu mol) were measured at the end of synthesis; total synthesis times were about 1 h 40 min.
引用
收藏
页码:31 / 36
页数:6
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