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

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-

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.