Luo Lei, Tang Ganghua, Tang Xiaolan
PET-CT Centre, Hunan Tumour Hospital, Changsha 410013,China.
Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2009 Nov;34(11):1151-6.
To study automated synthesis of 2-[(18)F]-fluoro-2-deoxy-D-glucose ((18)F-FDG) via on-column hydrolysis.
Automated synthesis of (18)F-FDG was performed by the on-column hydrolysis procedure in TRACERlab FXF-N synthesizer. (18)F-FDG injection was obtained via nucleophilic fluorination of 1, 3, 4, 6-tetra-O-acetyl-2-O-trifluoromethanesulfony-beta-D-mannopyranose as the precursor molecule with (18)F-fluoride, hydrolysis of the (18)F-labeled intermediate on SEP-PAK C18 cartridges with 2 mol/L NaOH solution, and purification and neutralization with SEP-PAK cartridges.
The uncorrected radiochemical yield of (18)F-FDG was more than 60% within the total synthesis time shorter than 20 min. The radiochemical purity of (18)F-FDG was above 99%.
On-column hydrolysis is simple and practical for the automated synthesis of (18)F-FDG. (18)F-FDG injection produced by this procedure can be used in clinical PET imaging.
研究通过柱上水解法自动合成2-[(18)F]-氟-2-脱氧-D-葡萄糖（(18)F-FDG）。
在TRACERlab FXF-N合成仪中采用柱上水解程序自动合成(18)F-FDG。以1,3,4,6-四-O-乙酰基-2-O-三氟甲磺酰基-β-D-甘露吡喃糖为前体分子，与(18)F-氟化物进行亲核氟化反应，然后用2 mol/L氢氧化钠溶液在SEP-PAK C18柱上水解(18)F标记的中间体，再用SEP-PAK柱进行纯化和中和，从而获得(18)F-FDG注射液。
在总合成时间短于20分钟的情况下，(18)F-FDG的未校正放射化学产率超过60%。(18)F-FDG的放射化学纯度高于99%。
柱上水解法对于自动合成(18)F-FDG简单且实用。通过该程序制备的(18)F-FDG注射液可用于临床PET成像。
