PET显像剂<sup>18</sup>F-FLT的合成条件优化

PET显像剂¹⁸F-FLT的合成条件优化

摘要: 以MTR-Nos-Boc-LT（3-N-Boc-5-DMTr-3-Nos-2-脱氧-β-D-胸腺嘧啶核苷）为前体，利用季铵盐为相转移催化剂，采用质子溶剂，摸索更优的¹⁸FLT合成方法。并就合成的¹⁸FLT进行肿瘤鼠的MicroPET扫描。研究结果显示，季铵盐可以取代K_2.2.2/K₂CO₃体系，将QMA柱上的¹⁸F洗脱，并且是很好的相转移催化剂，氟化反应中加入质子溶剂，¹⁸FLT的放化纯度大于95%，不矫正合成效率为50%。

Abstract: 3’-deoxy-3’-¹⁸F-fluorothymidine(¹⁸F-FLT) was synthesised with MTR-Nos-Boc-LT as precursor, uatemary ammonium salt as phase transfer catalyst, and buffer solution as neutralization solution. MicroPET imaging of A549 tumor in nude mice bearing tumor xenografts was performed by ¹⁸F-FLT. The results showed that uatemary ammonium salt is a good phase transfer catalyst, and can replace K_2.2.2/K₂CO₃ and elute ¹⁸F completely from QMA. The radiochemical purity was over 95% and the yield at EOS(end of synthesis)was 50%(uncorrected).