Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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The rapid synthetic strategy of [11C]PIB via disposable column cartridge purification

  • Jihye Lee (Neuroscience Research Institute, Gachon University) ;
  • Yansheng Li (PET-CT Center, Tianjin Medical University General Hospital) ;
  • Sang-Yoon Lee (Neuroscience Research Institute, Gachon University) ;
  • Tatsuo Ido (Neuroscience Research Institute, Gachon University)
  • Received : 2020.12.23
  • Accepted : 2020.12.29
  • Published : 2020.12.31
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Abstract

PIB is the first amyloid plaque PET image tracer reported for the first time in 2003, and is considered to be the best and is still being utilized due to its very high uptake and kinetic properties. Initially, it was synthesized by radioisotope labeling using a precursor containing a methoxy methyl protection group, but now it is synthesized using a 6-OH precursor that can be easily synthesized in one step using [11C]methyl triflate. Carbon-11 has several limitations in clinical studies using PET because its half-life is as short as 20 minutes. In this study, in order to overcome the difficulty of this half-life, a rapid method using Sep-Pak was adopted instead of HPLC purification to significantly reduce the burden of the purification process and attempted synthesis. As a result, the synthesis time was shortened by more than 50%, and the yield of the final compound was higher than the previous result and showed relatively high specific radioactivity, confirming that it is a strategic method with high applicability for various precursors having primary amines.

Keywords

Acknowledgement

본 연구는 보건복지부의 재원으로 한국보건산업진흥원의 보건의료기술연구개발사업 지원 (H I14C1135 )과 과학기술정보통신부의 재원으로 한국연구재단의 해외고급과학자초빙사업 (2018H1D3A2000959)에 의해 이루어짐.

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