Gd(Ⅲ)-DOTA类磁共振成像造影剂的合成策略与进展  

Synthetic Strategies and Progress of Gd(Ⅲ)-DOTA Derivatives Used as MRI Contrast Agents

作　　者：张元红 王艳芳[1] 万福贤[1] ZHANG Yuan-hong;WANG Yan-fang;WAN Fu-xian(College of Chemistry and Material Science,Shandong Agricultural University,Taian 271018,China)

机构地区：[1]山东农业大学化学与材料科学学院,山东泰安271018

出　　处：《化学试剂》2022年第10期1421-1432,共12页Chemical Reagents

基　　金：山东省自然科学基金项目(ZR2020MB011)。

摘　　要：近年来,基于钆(Ⅲ)的磁共振成像造影剂(GBCAs)受到了前所未有的挑战,迫切需要开发更安全、更惰性、靶向性、生化响应性钆(Ⅲ)基造影剂。由于环状多胺多羧类配体(如DOTA)更易于被功能性基团修饰,且其钆(Ⅲ)配合物比线性多胺多羧类钆(Ⅲ)配合物(如Gd-DTPA)具有更高的热力学稳定性和动力学惰性,因此在研发新型钆(Ⅲ)基造影剂领域备受青睐。以典型的DOTA类双功能造影剂配体(BFCAs)的设计、合成及应用为主线,重点介绍Gd-DOTA类造影剂的合成策略与进展。In recent years unprecedented challenges have arisen for gadolinium(Ⅲ)-based contrast agents(GBCAs),and there is an urgent need to develop safer,more inert,targeted,and bioresponsive GBCAs.Macrocyclic polyamine polycarboxylic ligands(e.g.,DOTA)are more easily modified by functional groups(e.g.,antibodies,peptides,aptamers)and their gadolinium(Ⅲ)-based complexes have higher thermodynamic stability and kinetic inertia when they are compared with those of gadolinium(Ⅲ)-based complexes with linear polyamine polycarboxylic ligands(e.g.,DTPA).Therefore,gadolinium(Ⅲ)-based complexes with macrocyclic polyamine polycarboxylic ligands are favored in the field of developing novel GBCAs.The synthetic strategies and recent progress of Gd(Ⅲ)-DOTA contrast agents were summarized by introducing the design and application of typical DOTA bifunctional contrast agent ligands(BFCAs).

关 键 词：磁共振成像(MRI) DOTA 钆(Ⅲ)配合物 双功能螯合试剂 合成策略 

分 类 号：O62[理学—有机化学]