Lee Y W, Iwashina T, Gati W P, Knaus E E, Wiebe L I
Int J Appl Radiat Isot. 1985 May;36(5):395-8. doi: 10.1016/0020-708x(85)90281-9.
The tritium-labelled acyclonucleoside, N-[2-(hydroxyethoxy)methyl]-5-[3H]methyluracil (3H-3), was synthesized for evaluation as a tumor diagnostic agent. 5-[3H]-Methyluracil, 3H-1, was converted to the 2,4-bis-trimethylsilyl intermediate which was coupled with 2-acetoxyethoxymethyl bromide to afford 1-[(2-acetoxyethoxy)methyl-5-[3H]methyluracil (3H-2). Treatment of 3H-2 with sodium methoxide in methanol afforded 3H-3 (specific activity 188 MBq mmol-1. The tissue distribution of 3H-3 was examined in male BDF1 mice bearing Lewis Lung (LL) carcinomas. Long bone exhibited the highest tumor: tissue ratios. The kidney contained the highest radioactivity level relative to the tumor. This suggested a major urinary route of excretion. The major radioactive blood component (89.21%) was found to have a biological half-life of 0.19 min. The title compound is unsuitable for use as a diagnostic agent for LL carcinoma because of low tumor uptake and rapid urinary elimination of injected radioactivity from the body.
合成了氚标记的无环核苷N-[2-(羟乙氧基)甲基]-5-[³H]甲基尿嘧啶(³H-3)，以评估其作为肿瘤诊断剂的性能。5-[³H]甲基尿嘧啶(³H-1)转化为2,4-双三甲基硅烷基中间体，该中间体与2-乙酰氧基乙氧基甲基溴偶联，得到1-[(2-乙酰氧基乙氧基)甲基]-5-[³H]甲基尿嘧啶(³H-2)。在甲醇中用甲醇钠处理³H-2得到³H-3(比活度为188 MBq mmol⁻¹)。在携带Lewis肺癌(LL)的雄性BDF1小鼠中研究了³H-3的组织分布。长骨显示出最高的肿瘤与组织比值。相对于肿瘤，肾脏中的放射性水平最高。这表明主要的排泄途径是通过尿液。发现主要的放射性血液成分(89.21%)的生物半衰期为0.19分钟。由于肿瘤摄取率低且注入体内的放射性从体内通过尿液快速消除，标题化合物不适合用作LL癌的诊断剂。
