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HETEROCYCLIC LIGANDS AND THE GADOLINIUM (III) COMPLEXES THEREOF WITH BIOMEDICAL APPLICATIONS

机译:杂环配体和THE(III)使其具有生物医学应用

摘要

The invention relates to compounds having general formula A and the paramagnetic complexes of Gd(III) and of other lanthanides thereof which are used as contrast agents for magnetic resonance imaging. More specifically, the invention relates to compounds having general formula A, wherein R1 and/or R2 are hydrogens, methyl groups, nitre groups and amino groups. The invention further relates to a method of obtaining said compounds from the corresponding bromoethylpyrazoles, comprising the following steps: 1) alkylation of the original amine 2) deprotection of the tert-butoxycarbonylamino groups 3) alkylation of the amino groups with methyl bromoacetate and, finally, 4) basic hydrolysis which produces the tetrasodium salt. The invention relates to complexes of Gd(III) and of other lanthanides derived from compounds having general formula A, to the method of obtaining said complexes and to the experimental and clinical use of same in the production of contrast agents for clinical diagnosis by means of magnetic resonance imaging.
机译:本发明涉及具有通式A的化合物及其Gd(III)及其其他镧系元素的顺磁性络合物,其用作磁共振成像的造影剂。更具体地,本发明涉及具有通式A的化合物,其中R 1和/或R 2是氢,甲基,腈基和氨基。本发明进一步涉及一种从相应的溴乙基吡唑类获得所述化合物的方法,其包括以下步骤:1)原始胺的烷基化2)叔丁氧基羰基氨基的脱保护基3)氨基与溴乙酸甲酯的烷基化,最后,4)碱性水解,生成四钠盐。本发明涉及Gd(III)和衍生自具有通式A的化合物的其他镧系元素的配合物,获得所述配合物的方法,以及该配合物在生产用于临床诊断的造影剂的方法中的实验和临床用途,所述造影剂通过以下方式进行:磁共振成像。

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