Cai Hancheng, Mangner Thomas J, Muzik Otto, Wang Ming-Wei, Chugani Diane C, Chugani Harry T
PET Center, Children's Hospital of Michigan, Detroit Medical Center , Detroit, Michigan 48201, United States ; Departments of Pediatrics, Radiology, and Neurology, Wayne State University School of Medicine , Detroit, Michigan 48201, United States ; Department of Radiology and Advanced Imaging Research Center, University of Texas Southwestern Medical Center , Dallas, Texas 75390, United States ; Department of Radiology and Advanced Imaging Research Center, University of Texas Southwestern Medical Center , Dallas, Texas 75390, United States.
PET Center, Children's Hospital of Michigan, Detroit Medical Center , Detroit, Michigan 48201, United States ; Departments of Pediatrics, Radiology, and Neurology, Wayne State University School of Medicine , Detroit, Michigan 48201, United States ; Departments of Pediatrics, Radiology, and Neurology, Wayne State University School of Medicine , Detroit, Michigan 48201, United States.
ACS Med Chem Lett. 2014 Aug 19;5(10):1152-5. doi: 10.1021/ml500285t. eCollection 2014 Oct 9.
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%.
（11）C-左乙拉西坦（（11）C-LEV）的多步制备通过一锅法放射性合成进行，在50±5.0分钟内放射化学产率为8.3±1.6%（n = 8）。简而言之，通过与氨孵育，将丙醛原位转化为丙-1-亚胺作为标记前体。无需进一步分离，亚胺与（11）C-HCN反应形成（11）C-氨基腈。然后将该粗品与4-氯丁酰氯反应，接着水解，通过手性高效液相色谱（HPLC）纯化后得到（11）C-LEV。（11）C-LEV的放射化学纯度和对映体纯度均>98%。
