18F亲电反应法直接标记氨基酸衍生物的研究

Study on direct electrophilic radiofluorination of amino acid derivatives

  • 摘要: 目的18F亲电反应法,研究一种方便、迅速的18F标记氨基酸衍生物的方法。方法 标记过程分三步进行:①加速器内20Ne (d,α)18F反应合成18F2气体;②18F2气体通过特制的反应柱,转化为CH3COO18F;③CH3COO18F与氨基酸衍生物直接反应,得到相应的标记物。结果 整个标记过程约为45min,放射性产额约60%,放射化学纯度>95%,pH值约为7,无菌性和热源实验均为阴性,这些结果保证了进一步动物实验和临床应用的可行性。结论 18F亲电反应法是一种简单易行的标记氨基酸衍生物的方法。

     

    Abstract: Objective To study an easy and fast method for the radiofluorination of amino acid derivatives.Methods The radiosynthesis procedure was divided into 3 steps:(1) Synthesis of 18F2gas by 20Ne (d,α)18F reaction in cyclotron. (2) By passing through a specific column, 18F2 gas was converted into CH3COO18F. (3) Fluorinated amino acid derivatives were synthesized by direct electrophilic reaction between amino acids and CH3COO18F.Results It took about 45 minutes to fulfill the whole synthesis procedure. The radioactivity yield rate, radiochemistry purity and pH value was about 60%, >95% and about 7 respectively. Both sterility and apyrogenicity test showed negative result. All these results guaranteed the following animal study and clinical application.Conclusion It is suggested that electrophilic radiofluorination reaction is an easy and fast way for the radiolabeling of amino acid derivatives.

     

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