超声波法合成2-~(18)F-2-脱氧-β-D-葡萄糖的初步研究
Synthesis of 2-~（18）F-fluoro-2-deoxy-β-D-glucose Using Ultrasound Promoted Method
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摘要: 采用超声波法合成 2 - 18F- 2 -脱氧 -β- D-葡萄糖 (18F- FDG), 以提高其合成效率。实验结果表明: F取代前体 2位上亲核反应进行的程度与相转移催化剂和温度有关。无相转移催化剂时, 84℃超声反应 10 min,亲核反应进行了 70 %;而在 10 mg的 K2.2.2存在下, 室温 (2 2℃ )下超声反应 10 min,亲核反应进行了 85 %, 在 84℃下超声反应 2 min,亲核反应进行了 95 %。同经典方法相比, 超声波合成法 18F-利用率提高了 10 %, 反应管的放射性吸附下降了 5 %。超声法合成效率 (EOS)为 6 0 %, 校正校率 (EOB)为 78%, 合成时间为 4 0 min。仅用一根 C- 18纯化柱纯化, 超声法合成的 18F- FDG中 18F-含量低于 1%。因此, 采用超声波法合成 18F- FDG可明显提高合成效率Abstract: fluoro 2 deoxy D glucose( 18 F FDG) is synthesized using ultrasound promoted method(UPM). The results show that the 2 nucleophilic substitution of F ion has relationship with phase transter catalyst and reaction temperature. The ultrasoundpromoted nucleophilic substitution reaction can finish 70% under 84 ℃ for 10 min without catalyst, 85% under 22 ℃ for 10 min with 10 mg catalyst and 95% under 84 ℃ for 2 min with 10 mg catalyst. Comparing with CTI method, the utilization of F ion of UPM improves 10% and the radioactivity absorption on vessel decreases 5%. The EOS is 60% and EOB is 78% in synthesis time of 40 min using UPM. The free F ion of 18 F FDG is lower than 1% after one C 18 colum purification. So 18 F FDG synthesis yield can be proved obviously using UPM.
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