高比度1,2-~2H睾丸酮的合成

SYNTHESIS OF1, 2-~3H TESTOSTERONE OF HIGH SPECIFIC RADIOACTIVITY

摘要: <正> 睾丸酮是人体内主要的雄性激素,正确地测定其含量,对于某些疾病的诊断、治疗及研究具有重要的意义。人体内睾丸酮的含量较低,多采用放射免疫分析法及竞争性蛋白结合分析法进行测定,因此需制备1,2-~3H睾丸酮。采用催化加成法,以1,2脱氢睾丸酮(以下均写成Δ~1睾丸酮)为前体,5％Pd-C为催化剂,二氧六环为溶剂,在氚气压为95800 Pa左右条件下进行催化加成反应,氚化时间为1.5小时,其反应式见图1。氚化产物首先采用硅胶纸薄层层析法,继而采用高压液体色谱法进行纯化,所得产品比活度达1887 GBq/mmol(51 Ci/mmol),放化纯度99％以上,已用于放免分析,用户满意,产品稳定,一年后,放化纯度仍达95.0％。

Abstract: 1,2-~3H testosterone of specific activity as high as 51 Ci/mmol, andradiochemical purity more than 99% has been prepared. The experimental condi-tions, such as reaction time, ratio of raw material catalyst and separation methodhave been studied. The product was separated by silica-paper TLC at first, then purified byhigh performance liquid chromatography. The product has good stability with apurity of 95% after one year storage.