新型非离子型单体碘造影剂的合成

Synthesis of Novel Nonionic Contrast Media of Iodin

目的合成4种新型非离子型X射线造影剂。方法以5-氨基-2,4,6-三碘异酞酰氯为起始原料,经氨烷基化、乙酰化或氯乙酰化、水解反应后制得粗品,再经XAD1600离子交换树脂和ODS柱层析纯化后得到纯品。结果产品经质谱、核磁共振确定分子结构后,做体外X射线造影,和市售碘海醇、碘佛醇造影效果比较。结论 4种新型非离子型单体造影剂造影效果显著,可以媲美目前市售造影剂的效果。

OBJECTIVE To synthesize four new types of contrast media. METHODS 5-amino-2,4,6-triiodoisophthaloyl chloride was used as starting material with a variety of processes including alkylation, acetylation or chloroacetylation and hydrolization to synthesize the crude product. Then the crude product was purified by ion exchange resin column chromatography and ODS chromatography to purify the title product. RESULTS The structure of the product was identified by MS and NMR, and the imaging effect was compared to iohexol and ioversol. CONCLUSION The imaging effect of four novel contrast media was significant and contrast effect is comparable with commercial products.