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- W2022188060 abstract "γ-Vinyl-γ-aminobutyric acid (GVG, Vigabatrin®), a suicide inhibitor of GABA-transaminase (GABA-T), has been suggested as a new drug for the treatment of substance abuse. In order to better understand its pharmacokinetics and potential side effects, we have developed a radiosynthesis of carbon-11 (t1/2=20 min) labeled GVG for positron emission tomographic (PET) studies. We report here a novel synthetic strategy to prepare the precursor and to efficiently label GVG with C-11. 5-Bromo-3-(carbobenzyloxy)amino-1-pentene was synthesized in five steps from homoserine lactone, including reduction and methylenation. This was used in a one-pot, two-step radiosynthesis. Displacement of bromide with no-carrier-added [11C]cyanide followed by acid hydrolysis afforded [1-11C]GVG with decay corrected radiochemical yields of 27±9% (n=6, not optimized) with respect to [11C]cyanide in a synthesis time of 45 min. Copyright © 2002 John Wiley & Sons, Ltd." @default.
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- W2022188060 date "2002-01-01" @default.
- W2022188060 modified "2023-10-18" @default.
- W2022188060 title "Novel synthesis of [1-11C]?-vinyl-?-aminobutyric acid ([1-11C]GVG) for pharmacokinetic studies of addiction treatment" @default.
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- W2022188060 doi "https://doi.org/10.1002/jlcr.544" @default.
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