使用由[11C]光气衍生的无水[11C]尿素自动放射性合成2-[11C]胸腺嘧啶核苷。

An automated radiosynthesis of 2-[11C]thymidine using anhydrous [11C]urea derived from [11C]phosgene.

作者信息

Steel C J, Brady F, Luthra S K, Brown G, Khan I, Poole K G, Sergis A, Jones T, Price P M

机构信息

MRC Cyclotron Unit, Imperial College School of Medicine, Hammersmith Hospital, London, UK.

出版信息

Appl Radiat Isot. 1999 Oct;51(4):377-88. doi: 10.1016/s0969-8043(99)00051-2.

DOI:10.1016/s0969-8043(99)00051-2

PMID:10464914

Abstract

2-[11C]Thymidine has been produced from [11C]methane via [11C]phosgene and [11C]urea. Anhydrous [11C]urea was prepared from [11C]phosgene by reaction with liquid ammonia. This novel approach avoids the problems associated with the synthesis of anhydrous [11C]urea from [11C]cyanide. A fully automated system based on a modular approach and under PLC control has been developed. The system provides 2-[11C]thymidine reliably and reproducibly for clinical PET studies. The radiosynthesis takes 45-50 min from [11C]methane and the average yield was 1.5-3.3 GBq (40-90 mCi). The specific radioactivity was typically in the range 29.6-51.8 GBq mumol-1 (0.8-1.4 Ci mumol-1) at EOS corresponding to 6-12 micrograms of stable thymidine. The radiochemical yield of 2-[11C]thymidine was ca. 14% from [11C]methane.

摘要

2-[¹¹C]胸腺嘧啶核苷是通过[¹¹C]甲烷经[¹¹C]光气和[¹¹C]尿素制备而成的。无水[¹¹C]尿素是由[¹¹C]光气与液氨反应制备的。这种新方法避免了与由[¹¹C]氰化物合成无水[¹¹C]尿素相关的问题。已开发出一种基于模块化方法并在可编程逻辑控制器（PLC）控制下的全自动系统。该系统能可靠且可重复地提供2-[¹¹C]胸腺嘧啶核苷用于临床正电子发射断层扫描（PET）研究。从[¹¹C]甲烷开始进行放射性合成耗时45 - 50分钟，平均产量为1.5 - 3.3吉贝可（40 - 90毫居里）。在合成结束时（EOS），比活度通常在29.6 - 51.8吉贝可/微摩尔（0.8 - 1.4居里/微摩尔）范围内，对应6 - 12微克稳定的胸腺嘧啶核苷。2-[¹¹C]胸腺嘧啶核苷的放射化学产率约为从[¹¹C]甲烷开始计算的14%。