全氘代双硫伦的合成

Synthesis of Disulfiram-d_(20)

以氘代二乙胺与二硫化碳为原料,四溴化碳诱导催化一步合成全氘代双硫伦,最终目标产物经质谱、核磁等表征确定,总收率为88.6%,化学纯度为99.2%,同位素丰度大于98%。该合成路线简单,原料易得,反应条件易于控制,满足其作为内标物在药理学、药代动力学等方面的应用。

In the presence of carbon tetrabromide,disulfiram-d20 was synthesized from diethylamine-d20 and carbon disulphide via one-pot reaction.The total yield was 88.6%,and the structure of the target compound was confirmed by MS and NMR.Its chemical purity was 99.2%and isotopic enrichment>98%.The synthetic route was simple and efficient,and all starting materials used in this study were commercially available.The compound could be used as an internal standard for pharmacology and pharmacological studies.