Jiang Xiao, Wang Xiao-Xiong, Lu Hao, Chen Shi-Rong, Xiao Ding-Qiong, Zhao Meng, Li Xiu-Li, Zhang Ge, Xu Guo-Hui, Cheng Zhu-Zhong
PET/CT Centre, Department of Radiology, Sichuan Cancer Hospital, Chengdu 610061, China.
Sichuan Da Xue Xue Bao Yi Xue Ban. 2017 Mar;48(2):295-298.
To synthesize 3'-deoxy-3'-¹⁸F-fluorotyhymidine)(¹⁸F-FLT) using CFN-MPS-200 automatic synthesis module, and evaluate its distribution in Wistar rats.
We used 3-N-Boc-5!d-O-dimethoxytrityl-3!d-O-nosyl-thymidine (Boc-FLT)-percursor as raw material to synthesize ¹⁸F-FLT without residual solvents. Its radiochemical purity was confirmed with radio-HPLC and thin layer chromatography (TLC). Normal Wistar rats were injected with F-FLT and underwent PET scanning.
The entire preparation procedure took about 60 min, which resulted in a radio chemical yield of (24±5)% (after attenuation correction, =20) and radiochemical purity of over 99%, with 1.11×10⁸ Bq/mL specific activity. The ¹⁸F-FLT solution was colorless and had a pH value between 7.0-8.0. ¹⁸F-FLT was mainly concentrated in the kidney, bladder, liver, bone marrow and Liver of normal Wistar rats.
Automated synthesis of ¹⁸F-FLT using CFN-MPS-200 is a stable method, with high yield, safety without solvent, and acceptable quality.
采用CFN-MPS-200自动合成模块合成3'-脱氧-3'-¹⁸F-氟胸苷（¹⁸F-FLT），并评估其在Wistar大鼠体内的分布。
以3-N-Boc-5'-O-二甲氧基三苯甲基-3'-O-亚硝基胸腺嘧啶核苷（Boc-FLT）前体为原料，合成无残留溶剂的¹⁸F-FLT。通过放射性高效液相色谱法和薄层色谱法（TLC）确认其放射化学纯度。对正常Wistar大鼠注射¹⁸F-FLT后进行PET扫描。
整个制备过程约需60分钟，放射化学产率为（24±5）%（衰减校正后，n = 20），放射化学纯度超过99%，比活度为1.11×10⁸Bq/mL。¹⁸F-FLT溶液无色，pH值在7.0 - 8.0之间。¹⁸F-FLT主要集中在正常Wistar大鼠的肾脏、膀胱、肝脏、骨髓和肝脏中。
使用CFN-MPS-200自动合成¹⁸F-FLT是一种稳定的方法，产率高，无溶剂安全，质量可接受。
