Radiosynthesis of <sup>11</sup>C‑Levetiracetam: A Potential Marker for PET Imaging of SV2A Expression

Abstract

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

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