Paper
An efficient new method for the synthesis of 3-[18 F]fluoro-4-aminopyridine via Yamada-Curtius rearrangement.
Published Feb 1, 2018 · F. Basuli, Xiang Zhang, P. Brugarolas
Journal of labelled compounds & radiopharmaceuticals
Q3 SJR score
15
Citations
0
Influential Citations
Abstract
4-Aminopyridine is a clinically approved drug to improve motor symptoms in multiple sclerosis. A fluorine-18-labeled derivative of this drug, 3-[18 F]fluoro-4-aminopyridine, is currently under investigation for positron emission tomography (PET) imaging of demyelination. Herein, the Yamada-Curtius reaction has been successfully applied for the preparation of this PET radioligand with a better radiochemical yield and improved specific activity. The overall radiochemical yield was 5 to 15% (n = 12, uncorrected) with a specific activity of 37 to 148 GBq/μmol (end of synthesis) in a 90 minute synthesis time. It is expected that this 1 pot Yamada-Curtius reaction can be used to prepare similar fluorine-18-labeled amino substituted heterocycles.
Study Snapshot
The Yamada-Curtius reaction efficiently synthesizes 3-[18 F]fluoro-4-aminopyridine for PET imaging of demyelination with improved radiochemical yield and specific activity in a 90-minute synthesis time.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
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