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发明公开
CN109912445A 碘海醇杂质F的合成方法及其在碘海醇杂质G、杂质H和杂质M合成中的应用 无效 - 驳回

碘海醇杂质F的合成方法及其在碘海醇杂质G、杂质H和杂质M合成中的应用
摘要：
本发明涉及一种碘海醇杂质的合成方法，特别涉及一种碘海醇杂质F的合成方法及其在碘海醇杂质G、杂质H和杂质M合成中的应用，属于医药技术领域。该方法是以5-硝基-1,3-苯二甲酸二甲酯（式2化合物）和2,3-二羟基丙胺为原料制备式3化合物，式3化合物与氢气还原反应制得式4化合物，式4化合物再与一氯化碘反应得到碘海醇杂质F。本发明以5-硝基-1,3-苯二甲酸二甲酯（式2化合物）为起始原料，合成5-氨基-N,N′-双（2,3-二羟基丙基）-二碘-1,3-苯二甲酰胺（式1化合物）再以化合物式1为起始原料合成杂质G、杂质H和杂质M，为碘海醇质量控制提供合格的杂质对照品。
摘要（英）：

The invention relates to a synthetic method of iohexol impurities, in particular to a synthetic method of an iohexol impurity F and an application thereof in synthesis of an iohexol impurity G, an impurity H and an impurity M and belongs to the technical field of medicines. The method comprises the steps as follows: a compound in formula 3 is prepared from raw materials including 5-nitro-1,3-dimethyl phthalate (a compound in formula 2) and 2,3-dihydroxyl propylamine, the compound in formula 3 and hydrogen are subjected to a reduction reaction to prepare a compound in formula 4, and the compound in formula 4 reacts with iodine chloride to obtain the iohexol impurity F. 5-amino-N,N'-bis(2,3-dihydroxypropyl)-diiodo-1,3-benzenedicarboxamide (a compound in formula 1) is synthesized from 5-nitro-1,3-dimethyl phthalate (the compound in formula 2) as the initial material, the impurity G, the impurity H and the impurity M are synthesized from the compound in formula 1 as the initial material, and qualified impurity reference substances are provided for quality control of iohexol.

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