Radiosynthesis of 11C-levetiracetam: A potential marker for PET imaging of SV2A expression

Hancheng Cai, Thomas J. Mangner, Otto Muzik, Ming Wei Wang, Diane C. Chugani, Harry T. Chugani

Research output: Contribution to journalArticle

26 Scopus citations

Abstract

The multistep preparation of 11C-levetiracetam (11C-LEV) was carried out by a one-pot radiosynthesis with 8.3 ± 1.6% (n = 8) radiochemical yield in 50 ± 5.0 min. Briefly, the propionaldehyde was converted to propan-1-imine in situ as labeling precursor by incubation with ammonia. Without further separation, the imine was reacted with 11C-HCN to form 11C-aminonitrile. This crude was then reacted with 4-chlorobutyryl chloride and followed by hydrolysis to yield 11C-LEV after purification by chiral high-performance liquid chromatography (HPLC). Both the radiochemical and enantiomeric purities of 11C-LEV were >98%.

Original languageEnglish (US)
Pages (from-to)1152-1155
Number of pages4
JournalACS Medicinal Chemistry Letters
Volume5
Issue number10
DOIs
StatePublished - Oct 9 2014

Keywords

  • Levetiracetam
  • carbon-11
  • positron emission tomography
  • synaptic vesicle protein 2A

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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