肿瘤增殖显像剂18F－FLT的合成和标记
Synthesis and Fluoro-Radiolabelling of Proliferation Imaging Agent 18F-FLT
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摘要: 为制备肿瘤增殖显像剂3'-脱氧-3’-氟胸腺嘧啶脱氧核苷（3’-deoxy-3’-fluorothymidine， 18F-FLT），合成了标记前体3-N-t-叔丁氧羰基-1-5’-O-(4, 4’-二甲氧基三苯甲基)-2’-脱氧-3’-O-(4-硝基苯磺酰基-β-1)-苏戊呋喃糖胸腺嘧啶脱氧核苷(N-BOC-FLT)并进行了标记。标记前体和各步合成中间体均经红外、核磁共振和质谱确证；于120 ℃进行亲核氟化反应，标记率为（35.2±5.8）%（经校正，n=2），用TLC和HPLC检测其放化纯度（RCP）大于95%，可满足临床研究的要求。
Abstract: Synthesis and fluoro-radiolabeling of proliferation imaging agent 3’deoxy3’-18F-fluorothymidine（18F-FLT）were reported. The chemical structure of the labeling precursor N-BOC-FLT and all its intermediates were verified by IR, MS and 1H NMR. Nucleophilic fluorination was proceeded at 120 ℃. Radiochemical yield is （35.2±5.8）% (n=2, decay corrected) and final radiochemical purity is above 95% determined by TLC and HPLC. Thereby it can be used preclinically.
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