氚标记阿魏酸和咖啡酸的合成
SYNTHESIS OF LABELLED COMPOUND OF FERULIC ACID AND CAFFEIC ACID WITH TRITIUM
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摘要: <正> 阿魏酸(Ferulic acid)和咖啡酸(Caffeic acid)分别是川芎和宁麻的有效成份。它们有良好的升白和止血作用,为了在动物体内进行药代动力学研究工作,需要氚标记阿魏酸和咖啡酸。但是它们的化学结构都具有不饱和双键,易发生亲电加成反应,这就不利于直接利用氚-氢交换方法。因此采用交换和合成相结合的方法,直接氚标记它们化学稳定的中间化合物,再进一步合成半定位的氚标记阿魏酸和咖啡酸。Abstract: Effective components of chinese traditional herbs consist of many compounds,but some of the compounds usually contain unsaturated carbon--carbon doublebonds. The unsaturated organic compounds ~3H--Ferulic acid and ~3H--Caffeic acidare prepared with their tritiated intermediates can be made by electric--dischangeexposure method, which ensures the compounds contaning double bonds do notbecome hydrogenated. ~3H--Ferulic acid is composed of ~3H--vanillin and Malonicacid, ~3H Caffeic acid is composed of ~3H--protocatechuyl aldehyde and Malonicacid. Specific activity of the products 0.2 mCi/mg. Radiochemicaly purity 90%.