Preparation method of ioversol intermediate

• Main Authors: PAN JIE, YAN XUEFENG, SHI YINGHUI, ZHU WANLI, SUN YAN
• Format: Patent
• Language: Chinese; English
• Published: 02.05.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a preparation method of an ioversol intermediate VI, which comprises the following steps of: sequentially performing chlorination, acylation, amidation and hydrolysis on a compound I, namely 5-aminoisophthalic acid serving as an initial raw material to obtain a compound of a formula V, namely N, N '-bis (2, 3-dihydroxy propyl)-5-(2-hydroxyacetamide) isophthalic diamide; the method provided by the invention is green and environment-friendly, the purity of the product can reach 99.52%, the cost of the raw materials applied in the whole method and the cost of the synthesis process are low, and the method is suitable for large-scale production in factories. 本发明公开了一种碘佛醇中间体VI的制备方法，该方法以化合物I：5-氨基间苯二甲酸为起始原料，依次经氯化、酰化、酰胺化、水解后，得到式V的化合物：N,N′-双(2，3-二羟基丙基)-5-(2-羟基乙酰胺)间苯二甲酰胺；再将式V碘化后，生成碘佛醇中间体VI：N,N′-双(2,3-二羟丙基)-5-羟基乙酰胺基-2,4,6-三碘间苯二甲酰胺：本发明的方法绿化环保，产品的纯度可达99.52％，整体方法应用的原料及合成工艺的成本低廉，适合工厂大规模化生产。