臨床供給のためのPET用薬剤の高効率合成と製剤化に関する研究
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概要
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Positron Emission Tomography (PET) is an advanced non-invasive technology used in the field of nuclear medicine for clinical diagnosis using radiotracers labeled with short-lived positron emitting radionuclides such as ^<11>C (halflife: 20.4 min), ^<13>N, ^<15>O and ^<18>F. The present study describes an efficient rapid synthesis method for [^<11>C] Phosgene ([^<11>C] COCl_2) which is an important potential precursor for preparation of PET radiopharmaceuticals. Catalytic oxidation of [^<11>C] CCl_4 using Fe_2O_3 powder mixed with Fe granules as an oxidizing agent was newly accomplished with a development of fully automated synthetic apparatus. Utilization of produced [^<11>C] COCl_2 provided a substantial synthesis of [2-^<11>C] thymine as a key intermediate for preparation of [2-^<11>C] thymidine, a PET tracer to evaluate cellular proliferation. Direct ring closure reaction of the alkali metal salt of β-(N-benzoyl-amino) methacrylamide with [^<11>C] COCl_2 readily proceeded under mild conditions to afford [2-^<11>C] thymine in fair yield reproducibly. By way of further application, a useful PET ligand for β-adrenoreceptors, S-(-)-[^<11>C] CGP-12177 (CGP) was synthesized in markedly high yield with high specific activity and radiochemical purity. CGP for intravenous injection was prepared in 25 min after BOB with a yield of 1.5±0.2 GBq. These results of quality control tests demonstrated that CGP preparation is suitable for routine clinical use. Thus, CGP-PET study has been newly added to clinical PET for cardiac functional investigation in Hokkaido University Hospital.
- 公益社団法人日本薬学会の論文
- 2006-09-01