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 language | English (US) |
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Pages (from-to) | 1152-1155 |
Number of pages | 4 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 5 |
Issue number | 10 |
DOIs | |
State | Published - Oct 9 2014 |
Keywords
- Levetiracetam
- carbon-11
- positron emission tomography
- synaptic vesicle protein 2A
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry