点击化学在三羰基铼标记2,2’-二吡啶甲基胺衍生物中的应用

The study on synthesis of di-(2-picolyl)amine analogs obtained via click chemistry and its labeling with fac-[Re(CO)3]+

摘要:

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）并通过“点击化学” 生成含有吡啶环的三齿螯合剂。2,2’-二吡啶甲基胺上的三个氮原子和三羰基铼进行配位生成冷标记产物，总产率大于75 %，冷标记产率大于90 %；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、羧基三个配位基团与三羰基铼水合物前体配位，总产率大于82 %，冷标记产率大于90 %。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。

Abstract:

Tridentate chelating agents containing pyridine rings were synthesized by click chemistry with alkyne (c) and azide (d) which are the derivatives of bis(pyridin-2-ylmethyl)amine. The cold labeling yields of the compounds synthesized by the three nitrogen atoms in these tridentate chelating agents and fac-[Re(CO)3(H2O)3]+ were more than 90 %, and the total yields were over 75 %, comparable to the yields of the compounds synthesized by fac-[Re(CO)3]+ and the tridentate chelating agents containing carboxyl, amino-group and nitrogen atom (N3) in the triazol ring which synthesized from 2-aminopent-4-ynoic acid were more than 90 % and 82 %. The tridentate chelating agents analogues which contain different pyridine rings and triazole compounds which contain amino and carboxyl could be potential radiolabeling ligands for fac-[188Re(CO)3(H2O)3] + as the bifunctional chelating agents.