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通过优化设计,合成了高产率的DTPA和DOTA配体.通过液相发散法制得第三代肽类树状大分子,其外围氨基分别用两种不同保护基团保护,且两种保护基团的个数比精确控制为18∶6,通过选择性脱去保护基团,其中一种氨基与DTPA、DOTA偶联,或与丁二酸酐反应,并与金属离子钆螯合,制得G3-18Gd-DTPA-6COOH,G3-18Gd-DOTA-6COOH两种肽类树枝状磁共振成像(MRI)分子探针.所合成化合物的结构通过1 H-NMR,13 C-NMR,ESI-TOF-MS表征.水相弛豫研究表明,2种肽类树状大分子MRI分子探针在水相中表现出了优良的弛豫效能,最高达12.53 L.mmol-1.s-1,是临床试剂Gd-DTPA的3倍.
By optimizing the design, high yields of DTPA and DOTA ligands were synthesized.The third-generation peptide dendrimer was prepared by liquid-phase diffusion method, the peripheral amino groups were protected by two different protective groups respectively, and the two protective groups The ratio of the number of precisely controlled 18: 6, by selective removal of protective groups, one of the amino group with DTPA, DOTA coupling, or with succinic anhydride reaction and chelation with metal ions gadolinium G3- 18Gd-DTPA-6COOH and G3-18Gd-DOTA-6COOH.The molecular structures of the synthesized compounds were characterized by1H-NMR, 13C-NMR and ESI-TOF-MS Characterization of water phase relaxation studies showed that the two peptide dendrimer MRI molecular probe showed excellent relaxation efficiency in the aqueous phase, up to 12.53 L.mmol-1.s-1, is a clinical reagent 3 times Gd-DTPA.