대한방사성의약품학회지 (Journal of Radiopharmaceuticals and Molecular Probes)

  • 제6권2호
  • /
  • Pages.69-74
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  • 2020
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  • 2384-1583(pISSN)
  • /
  • 2508-3848(eISSN)
대한방사성의약품학회 (Korean Society of Radiopharmaceuticals and Molecular Probes)
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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)
  • 투고 : 2020.12.23
  • 심사 : 2020.12.29
  • 발행 : 2020.12.31
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초록

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.

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과제정보

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

참고문헌

  1. Mathis CA, Wang Y, Holt DP, Huang GF, Debnath ML, Klunk WE. Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem. 2003 Jun 19;46(13):2740-54.
  2. Klunk WE, Engler H, Nordberg A, Wang Y, Blomqvist G, Holt DP, Bergstrom M, Savitcheva I, Huang GF, Estrada S, Ausen B, Debnath ML, Barletta J, Price JC, Sandell J, Lopresti BJ, Wall A, Koivisto P, Antoni G, Mathis CA, Langstrom B. Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B. Ann Neurol. 2004 Mar;55(3):306-19.
  3. Wilson, A.A., Garcia, A., Chestakova, A., Kung, H. and Houle, S. (2004), A rapid one-step radiosynthesis of the β-amyloid imaging radiotracer N-methyl-[11C]2-(4'-methylaminophenyl)-6-hydroxybenzothiazole ([11C]-6-OH-BTA-1). J Label Compd Radiopharm, 47: 679-682.
  4. Fedorova, O., Kuznetsova, O., Stepanova, M. et al. A facile direct nucleophilic synthesis of O-(2-[18F] fluoroethyl)-L-tyrosine ([18F]FET) without HPLC purification. J Radioanal Nucl Chem 301, 505-512 (2014).
  5. Fedorova O, Nikolaeva V, Krasikova R. Automated SPE-based synthesis of 16α-[18F]fluoroestradiol without HPLC purification step. Appl Radiat Isot. 2018 Nov;141:57-63.