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Copper-Mediated Late-Stage Iodination and 123I-Labelling of Triazole-benzimidazole Bioactives
Synlett ( IF 1.7 ) Pub Date : 2018-04-19 , DOI: 10.1055/s-0036-1591985
Jørn Hansen 1 , Richard Fjellaksel 1, 2, 3 , Rune Sundset 2, 4 , Patrick Riss 5, 6, 7
Affiliation  

The copper-mediated azide-alkyne cycloaddition has been studied to achieve late-stage introduction of iodine onto novel triazole-benzimidazole Gonadotropin Releasing Hormone (GnRH)-receptor antagonists. Moreover, the reaction conditions can affect a direct regioselective C–H iodination of the benzimidazole, leading to a range of novel iodo-analogues. The methodologies are powerful strategies for late-stage 123 I-labelling of complex bioactives. Our investigations have generated two highly promising 123 I-labelled radiotracer candidates that retain high affinities for the GnRH-receptor.

中文翻译:

三唑-苯并咪唑生物活性物质的铜介导后期碘化和 123I 标记

已经研究了铜介导的叠氮化物-炔环加成反应,以实现后期将碘引入新型三唑-苯并咪唑促性腺激素释放激素 (GnRH)-受体拮抗剂。此外,反应条件会影响苯并咪唑的直接区域选择性 C-H 碘化,从而产生一系列新型碘类似物。这些方法是复杂生物活性物质后期 123 I 标记的有力策略。我们的调查产生了两个非常有希望的 123 I 标记的放射性示踪剂候选物,它们保留了对 GnRH 受体的高亲和力。
更新日期:2018-04-19
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