Teng Bao, Wang Shizhen, Fu Zhe, Dang Yonghong, Wu Zhanhong, Liu Liqin
Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100730, China.
Appl Radiat Isot. 2006 Feb;64(2):187-93. doi: 10.1016/j.apradiso.2005.07.017. Epub 2005 Aug 29.
To facilitate clinical studies with [18F]FLT, we modified 2-vessel [18F]FDG synthesis module (manufactured by CTI) to produce [18F]FLT. Three thymidine derivatives were used as precursors for [18F]FLT synthesis. Among these precursors, 3-N-t-butoxycarbonyl-[5'-O-(4,4'-dimethoxytrityl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)-beta-D-threopentofuranosyl]thymine (thymidine derivative II) gave the best radiochemical yield (37.9%) when the reaction was carried out at 140 degrees C for 5 min. This semiautomatic synthesis system was not only simple and convenient, but also showed good reproducibility. The total synthesis time was 50 minutes from the end of bombardment (EOB) by the use of this modified synthesizer (including the manual process).
为便于开展[18F]FLT的临床研究，我们对两管[18F]FDG合成模块（由CTI制造）进行了改造以制备[18F]FLT。三种胸苷衍生物用作[18F]FLT合成的前体。在这些前体中，当反应在140℃下进行5分钟时，3-N-叔丁氧羰基-[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-D-苏式戊呋喃糖基]胸腺嘧啶（胸苷衍生物II）给出了最佳的放射化学产率（37.9%）。这种半自动合成系统不仅简单方便，而且具有良好的重现性。使用这种改造后的合成仪（包括手工操作过程），从轰击结束（EOB）起的总合成时间为50分钟。
