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本文对四种人体甾族生殖激素进行了放射性多位氚标记的研制。 1.[1,2,6,7-~3H]孕酮,[1,2,6,7,-~3H]睾丸酮及[1,2,6,7-~3H]皮质醇的合成。前体~(1,6)Δ-孕酮,~(1,6)Δ-睾丸酮及~(1,6)Δ-皮质醇分别溶于二氧六环,用催化剂10％钯碳经催化加氚后,除去催化剂及不稳氚,经硅胶纸层析分离纯化,放射性产物的化学量与浓度用分光光度计在λ_(max)为241nm波长时测定,其平均摩尔消光系数分别为16850,14550及15400。用液闪测得,氚标记物的总比活度分别为3.56、3.04、3.36TBq/mmol。用放射性硅胶纸层析及高效液相色谱法测得氚标记物放化纯度均大于98％。为保证分子中1.2及6.7位的双键被氚化,必须严格控制反应条件。
In this paper, four kinds of human steroid hormones were developed for radioactive tritium labeling. 1. [1,2,6,7- ~ 3H] progesterone, [1,2,6,7, - ~ 3H] testosterone and [1,2,6,7- ~ 3H] cortisol synthesis. Precursor ~ (1,6) Δ-progesterone, ~ (1,6) Δ -testosterone and ~ (1,6) Δ-cortisol were dissolved in dioxane and catalyzed by 10% After tritium removal, the catalyst and unstable tritium were removed and purified by chromatography on silica gel. The chemical quantity and concentration of the radioactive products were measured with a spectrophotometer at λ max of 241 nm. The average molar extinction coefficients were 16850 and 14550 And 15400. Measured by liquid flash, the total specific activity of tritiated labels was 3.56, 3.04 and 3.36TBq / mmol, respectively. Radioactive silica gel chromatography and high performance liquid chromatography tritium labeled radiochemical purity were greater than 98%. In order to ensure that the double bonds at positions 1.2 and 6.7 of the molecule are tritiated, the reaction conditions must be strictly controlled.