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′{luorothymidine,^18F-FLT),合成了标记前体3-N-t-叔丁氧羰基-1[5’0-(4,4′-二甲氧基三苯甲基)-2′-脱氧-3′-0-(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%,可满足临床研奔的要求。
Synthesis and fluoro-radiolabeling of proliferation imaging agent 3′-deoxy-3′-1-18 F] 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 radioehemical purity is above 95% determined by TLC and HPLC. Thereby it can be used preelinically.