Facile synthesis of carbon-11-labeled arylpiperazinylthioalkyl derivatives as new PET radioligands for imaging of 5-HT 1AR

Mingzhang Gao, Min Wang, Qi Huang Zheng

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

Carbon-11-labeled arylpiperazinylthioalkyl derivatives, 2-((4-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]oxazole ([ 11C]5a), 2-((4-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)butyl)thio)-5,7-dimethylbenzo[d]oxazole ([ 11C]5c), 2-((4-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]thiazole ([ 11C]5e), 2-((6-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]oxazole ([ 11C]5g), 2-((6-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)hexyl)thio)-5,7-dimethylbenzo[d]oxazole ([ 11C]5i), and 2-((6-(4-(2-[ 11C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]thiazole ([ 11C]5k), were prepared from their corresponding phenol precursors with [ 11C]CH 3OTf through O-[ 11C]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 [ 11C]CO 2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 23min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 277.5±92.5GBq/μmol (n=5).

Original languageEnglish (US)
Pages (from-to)498-504
Number of pages7
JournalApplied Radiation and Isotopes
Volume70
Issue number3
DOIs
StatePublished - Mar 2012

Keywords

  • Carbon-11-labeled arylpiperazinylthioalkyl derivatives
  • Imaging
  • Positron emission tomography (PET)
  • Radioligands
  • Serotonin-1A receptor (5-HT R)

ASJC Scopus subject areas

  • Radiation

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