Molecular Design and Synthetic Strategy toward Development of PET Probes

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  • Niwa Takashi
    Graduate School of Pharmaceutical Sciences, Kyushu University RIKEN Center for Biosystems Dynamics Research (BDR) Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU)
  • Hosoya Takamitsu
    RIKEN Center for Biosystems Dynamics Research (BDR) Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU)

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  • PETプローブ開発を指向した分子設計と合成戦略
  • PET プローブ カイハツ オ シコウ シタ ブンシ セッケイ ト ゴウセイ センリャク

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<p>The positron emission tomography (PET) is one of the imaging technologies that allows for visualization of the behavior of a bioactive compound labeled with a positron emission nuclide, generally called a PET probe. To date, many (radio) chemists have developed various methods to introduce a short-lived PET nuclide, such as carbon-11 or fluorine-18, and expanded the available range of chemical structures of small molecular-based PET probes. However, the number of useful PET probes for life science research is still limited. This is mainly due to the insufficient range of available radiolabeling reactions, limiting the synthesizable chemical structures of PET probes. Furthermore, the densely functionalized complex structure of the compounds in interest impedes the preparation of radiolabeling precursors. To address these issues, we have proposed two strategies; one is the molecular renovation strategy that enables expeditious preparation of labeling precursors, and the other is the mimic strategy for designing a radiolabelable chemical structure for PET probe development. This account describes these two concepts and our recent efforts to realize them by developing various borylations and radiolabeling reactions.</p>

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