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    • 10. 发明申请
    • PROCESS FOR PRODUCING 1, 4, 7, 10-TETRAAZACYCLODODECANE-1, 4, 7, 10-TETRAACETIC ACID AND COMPLEXES THEREOF
    • 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-十四酸及其复合物的制备方法
    • WO2014114664A1
    • 2014-07-31
    • PCT/EP2014/051217
    • 2014-01-22
    • AGFA HEALTHCARE
    • BUFFEL, DiederikGANORKAR, RakeshBURT, JenniferBOI, Xavier
    • C07D457/04
    • C07D257/02A61K49/108C07D457/04
    • The present invention relates to a process for producing 1, 4, 7, 10-tetraazacyclododecane-1, 4, 7, 10-tetraacetic acid (DOTA) including salts and hydrates thereof of general formula (I) from the respective cyclen. Said process further involves the use of cationic- and anionic exchange resins and solvent treatments to remove the organic and inorganic contaminants. Any cations present in the raw DOTA or other contaminants resulting from the reaction of cyclen are largely reduced in early stages of the process allowing to obtain good yields of DOTA in a purified grade and in an easier and reliable way. The present invention is thus useful for the production of DOTA, of macrocyclic compounds comprising metal ions complexes thereof and of compositions comprising said macrocyclic compounds that can be used as contrast agents for magnetic resonance imaging.
    • 本发明涉及从相应的环烯烃生产包括其通式(I)的盐和其水合物的4,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA)的方法。 所述方法还涉及使用阳离子和阴离子交换树脂和溶剂处理来除去有机和无机污染物。 存在于原始DOTA中的任何阳离子或由环化物反应产生的其它污染物在该方法的早期阶段大大降低,从而在纯化级别中以更容易和可靠的方式获得良好的DOTA产率。 因此,本发明可用于生产DOTA,其包含其金属离子络合物的大环化合物和包含可用作磁共振成像造影剂的所述大环化合物的组合物。