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Appl Radiat Isot. 2012 Mar;70(3):498-504. doi: 10.1016/j.apradiso.2011.11.034. Epub 2011 Nov 25.

Facile synthesis of carbon-11-labeled arylpiperazinylthioalkyl derivatives as new PET radioligands for imaging of 5-HT1AR.

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  • 1Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, 46202-2111, USA.


Carbon-11-labeled arylpiperazinylthioalkyl derivatives, 2-((4-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]oxazole ([(11)C]5a), 2-((4-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)butyl)thio)-5,7-dimethylbenzo[d]oxazole ([(11)C]5c), 2-((4-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]thiazole ([(11)C]5e), 2-((6-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]oxazole ([(11)C]5g), 2-((6-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)hexyl)thio)-5,7-dimethylbenzo[d]oxazole ([(11)C]5i), and 2-((6-(4-(2-[(11)C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]thiazole ([(11)C]5k), were prepared from their corresponding phenol precursors with [(11)C]CH(3)OTf through O-[(11)C]methylation and isolated by a simplified solid-phase extraction (SPE) method using a Sep-Pak Plus C18 cartridge in 50-60% (n=5) radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 23 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 277.5 ± 92.5 GBq/μmol (n=5).

Copyright © 2011 Elsevier Ltd. All rights reserved.

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