【摘要】 碘普罗胺是一种常用的碘造影剂。以3—氨基—5—[[(2,3—二羟基丙基)氨基]羰基]苯甲酸为起始原料，通过6步反应合成常用的碘化造影剂碘普罗胺。将S-1碘化后，将所得的三酰中间体M-1进行O-Ac保护，随后进行酰胺化，生成2-甲氧基乙酰基。然后通过酸性氯化物中间体M-4实现第二次酰胺化。最后，使用NaOH水溶液将两个乙酰保护基团水解断裂。再经过大孔吸附树脂和阴阳离子树脂对反应液进行一次纯化，得到碘普罗胺粗品，然后在乙醇溶剂中重结晶进一步纯化。该方法6步反应的总收率为25.6%。同时合成产物经核磁共振氢谱(~1H-NMR)结构确证。该合成工艺简单易操作，适合应用于工业化生产。该合成工艺简单、易操作，不使用昂贵原料，适合应用于工业化生产。更多还原

【Abstract】 A modified synthesis of iopromide, a commonly used iodinated contrast agent, was accomplished in six steps starting from cheap 3-amino-5-[[(2,3-dihydroxypropyl)amino]carbonyl]benzoic acid.Upon iodination of S-1,the resulting triiodo intermediate M-1 was subjected to O-Ac protection and subsequent amidation to introduce 2-methoxy acetyl group.The second amidation was then achieved through an acid chloride intermediate M-4.Finally, the two acetyl protection groups were cleaved by hydrolysis with aqueous NaOH.The crude iopromide, which was obtained upon treatment with macroporous adsorption resin and anioncation resin, was further purified by recrystallization in ethanol solvent.The overall yield of this six-step sequence was 25.6%,and the final product was confirmed by ~1H-NMR.This synthesis process proved to be straightforward, easy to operate, and suitable for industrial production.更多还原