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首先合成了2,2’-二吡啶甲基胺的炔基衍生物(c)和叠氮衍生物(d),再通过“点击化学”生成了两种含有吡啶环的三齿螯合剂。2,2’-二吡啶甲基胺上的3个氮原子和三羰基铼进行配位生成冷标记产物,点击化学产率大于90%,冷标记率大于80%。以炔丙基甘氨酸为原料,合成了1,2,3-三唑化合物,利用三唑环上的(N3)氮原子和氨基、羧基3个配位基团与三羰基铼水合物前体配位,点击化学产率大于90%,冷标记率大于90%。所合成的两种含有吡啶环的三齿配体和含有氨基酸的三唑化合物均可作为双功能螯合剂,是很有潜力的三羰基铼水合物放射性前体的标记配体。
First, the alkynyl derivatives (c) and the azide derivatives (d) of 2,2’-dipyridylmethylamine were synthesized and then two pyridinium ring-containing tridentate chelators were generated by “click chemistry” . The three nitrogen atoms on 2,2’-dipyridyl methylamine coordinate with rhenium tricarbonyl to generate the cold labeled product with a click chemical yield greater than 90% and a cold labeling rate greater than 80%. 1,2,3-triazole compounds were synthesized from propargylglycine. By using the (N3) nitrogen atom on the triazole ring and the amino group, three coordination groups of the carboxyl group and the precursor of tricarbonyl rhenium hydrate Bit, click chemical yield greater than 90%, cold mark rate greater than 90%. The two synthesized pyridine ring-containing tridentate ligands and amino acid-containing triazole compounds can be used as a bifunctional chelating agent, is a potential tricarbonyl rhenium hydrate radioactive precursor labeled ligand.