自动化合成2-^(18)F-β-D-脱氧葡萄糖及其质量控制

Automated Synthesis and Quality Control of 2-[^(18)F]-Fluoro-2-Deoxy-D-Glucose

采用TRACERlab FXF-N自动化合成装置制备了肿瘤显像剂2-18F-β-D-脱氧葡萄糖(18F-FDG)。以三氟甘露糖为前体,在同一反应瓶中经过亲核氟化、氢氧化钠水解两步反应,然后用小柱分离纯化制备了18F-FDG注射液。同时还研究了亲核取代氟化反应体系中的含水量和前体三氟甘露糖的用量对合成效率的影响。结果表明,18F-FDG总合成时间约25 min,未校正18F衰变情况下,放射化学产率约55%,放射化学纯度大于95%。

Automated synthesis of 2 - [^18F] - fluoro - 2 - deoxy - D - glucose （ ^18F- FDG） was performed by two- stop reaction procedure at TRACERlab FXF - N system, ^18F- FDG injection was obtained via two - step reaction including nucleophilic fluorination of the precursor 1,3,4, 6 - tetra - O - acetyl - 2 - O - trifuoromethanesulfo- ny-β- D -mannopyranose with ^18F- fuoride and hydrolysis with NaOH in the same reaction vessel, and subsequently purificated with Sep - Pak cartridges. The influence factors of synthesis yield were investigated, ^18F - FDG was performed with the uncorrected radiochemical yield about 55% and radiochemical purity above 95% within the total synthesis time about 25 min.