新型非离子型单体碘造影剂的合成-中国现代应用药学.pdfVIP

 杨天帅 1 ，王海燕 2 ，韩大雄 1*(1. 361005 2. 361005) 合成 4 种新型非离子型 X 射线造影剂。 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。 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。 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。 造影剂；碘海醇；碘佛醇 R914.2 B 1007-7693(2013)08-0843-05 Synthesis of Novel Nonionic Contrast Media of Iodin 1 2 1* YANG Tianshuai , WANG Haiyan , HAN Daxiong (1.School of Pharmaceutical Sciences, Xiamen University, Xiamen 361005, China; 2.Third Institute of Oceanography, State Oceanic Administration, Xiamen 361005, China) ABSTRACT: 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. KEY WORDS: contrast media; iohexol; ioversol X [1] CT 1 3--1,2-2- [2] -1,3-3--1,2-N- -2,3- X ( ) XAD1600 () ODS( [3] ) HP 1200 Agilent 6320 Bruker AV-400 5 1000/GFS X 2,3- 2