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通过Cu(I)催化的点击化学合成一种放射性碘标记化合物,建立一套新的放射性碘标记的方法,该方法温和、快速、高效。结果显示在有机相反应中,通过点击化学反应5-碘(-125/131I)-1,2,3-三唑化合物在24 h内合成,放射化学产率达到13%。但是在水相中,点击化学标记生物分子RGD的放射化学产率为0。原因是在水相中,Cu(I)催化作用使得氢离子和碘离子发生了交换反应,没有足够的放射性碘配体与RGD发生偶联。本文还提出了在反应溶剂为有机相和水相的条件下Cu(I)催化该环加成反应的不同反应机制。
A radioactive iodine labeled compound was synthesized by click chemistry catalyzed by Cu (I) to establish a new set of radioactive iodine labeling method which is mild, rapid and efficient. The results showed that in the organic phase reaction, the radiochemical yield reached 13% by clicking the chemical reaction 5-iodine (-125 / 131I) -1,2,3-triazole compound within 24 h. However, in the aqueous phase, the radiochemical yield of click chemistry labeled biomolecule RGD is zero. The reason is that Cu (I) catalyzes the exchange reaction of hydrogen ions and iodide ions in the aqueous phase, and there is not enough radioactive iodine ligand to couple with RGD. This paper also proposed different reaction mechanism of Cu (I) catalysing the cycloaddition reaction under the conditions of reaction solvent of organic phase and aqueous phase.