ACS Medicinal Chemistry Letters 2014-10-09

Radiosynthesis of (11)C-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

文献索引：ACS Med. Chem. Lett. 5(10) , 1152-5, (2014)

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摘要

The multistep preparation of (11)C-levetiracetam ((11)C-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 (11)C-HCN to form (11)C-aminonitrile. This crude was then reacted with 4-chlorobutyryl chloride and followed by hydrolysis to yield (11)C-LEV after purification by chiral high-performance liquid chromatography (HPLC). Both the radiochemical and enantiomeric purities of (11)C-LEV were >98%.

相关化合物

  • 4-氯丁酰氯

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