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碘海醇的制备工艺优化
引用本文:秦海芳.碘海醇的制备工艺优化[J].五邑大学学报(自然科学版),2013(4):40-43.
作者姓名:秦海芳
作者单位:常州工程职业技术学院制药与生物工程技术系,江苏常州213164
摘    要:以5-硝基-N,N’-双(2,3-二羟丙基)-1,3.苯二甲酰胺为原料,通过还原、碘代、酰化、烷基化反应制备碘海醇.优化了合成工艺中碘代反应和烷基化反应步骤:在碘代反应中,用碘化钾为碘源、亚氯酸钠为氧化剂代替氯化碘作为碘化试剂;在N-烷基化反应中,用二乙二醇甲醚代替1,2.丙二醇.探讨了物料比、温度等因素对反应的影响,确定了最佳反应条件,总收率达49.4%,产品结构经光谱确证.

关 键 词:造影剂  碘海醇  碘代反应  烷基化反应

Optimization of the Preparation of Iohexol
QIN Hai-fang.Optimization of the Preparation of Iohexol[J].Journal of Wuyi University(Natural Science Edition),2013(4):40-43.
Authors:QIN Hai-fang
Institution:QIN Hai-fang (Department of Pharmaceutical-Technology and Biological Engineering, Changzhou Institute of Engineering Technology, Changzhou 213164, China)
Abstract:With 5-nitro-N, N'-bis (2, 3-dihydroxypropyl)-1 and 3-benzene dicarboxamide as raw material, iohexol was obtained through reduction, iodo, acylation, and alkylation. The steps of Iodination and alkylation reaction in the synthesis reaction were optimized: In the iodination, potassium iodide was used as a source of iodine and sodium chlorite was used as iodination reagent in place of iodine chloride; in N- alkylation reaction, diethylene glycol ether was used in place of 1,2-propylene glycol. The effects of material ratio and temperature on the reaction were explored and the optimum reaction conditions were determined. The total yield was 49.4% and the prodluct structure was confirmed by means of spectral composition.
Keywords:contrast agent  iohexol  iodination reactioia  alkylation reaction
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