葡萄糖转运蛋白显像剂6-~(18)FDG的制备及在小鼠体内的分布

为了研究正电子核素18F标记的葡萄糖转运蛋白显像剂6-18氟-6-脱氧葡萄糖的制备及在小鼠体内的生物学分布, 以D-葡萄糖为起始原料, 经过丙酮和苯甲醛对1,2,3,5位羟基的定位保护, 然后用对甲苯磺酰氯和6位的羟基反应得到能被18F-进攻的离去基团, 最后用18F-离子通过亲核取代反应实现对葡萄糖6位的氟代标记; 反应中间体用NMR和MS表征, 最终产物用标准品6-19FDG在HPLC下对照确认, 测定放化纯度, 观察其在小鼠体内的生物学分布. 6-18氟-6-脱氧葡萄糖的放射性标记过程需35 min(从加速器轰击结束算起), 放化产率70%±5%(校正后, n=5), 放化纯度>95%. 小鼠体内的生物学分布表明, 各个器官在1.0 min达到峰值, 然后逐渐平衡. 初步研究结果表明, 6-18FDG是一种很有价值的葡萄糖转运蛋白显像剂, 为以后的体内外研究及活体显像奠定了基础.

One-pot Synthesis and Biodistribution of 6-[~(18)F]Fluoro-6-deoxy-D-glucose(6-~(18)FDG) as Potential Glucose Transport Imaging Agent

For the development glucose transport imaging,a radioactive glucose analogue was synthesized and evaluated.A glucose analogue,6-[18F]fluoro-6-deoxy-D-glucose(6-18FDG),was prepared in two steps with one-pot synthesis from [18F]fluoride and tosyl-precursor.Starting with D-glucose,the D-glucose was reacted with acetone and benzaldehyde to protect hydoxy,then reacted with p-toluenesulfonyl choride(TsCl)to get the tosyl-precursor.All the intermediates were identified with NMR and MS.The total radiosysthesis spen...