A new fluorine‐containing azadibenzocyclooctyne (ADIBO‐F) was designed using a synthetically accessible pathway. The fluorine‐18 prosthetic group was prepared from its toluenesulfonate precursor and isolated in 21–35 % radiochemical yield in 30 minutes of synthetic time. ADIBO‐F has been incorporated into azide‐functionalized, cancer‐targeting peptides through a strain‐promoted alkyne–azide cycloaddition with high radiochemical yields and purities. The final products are novel peptide‐based positron emission tomography (PET) imaging agents that possess high affinities for their targets, growth hormone secretagogue receptor 1a (GHSR‐1a) and gastrin‐releasing peptide receptor (GRPR), with IC₅₀ values of 9.7 and 0.50 nm, respectively. This is a new and rapid labelling option for the incorporation of fluorine‐18 into biomolecules for PET imaging.

中文翻译：

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一个紧凑且可合成合成的氟18标记的环辛炔假体，用于通过无铜点击化学标记生物分子

使用可合成的途径设计了一种新的含氟氮杂二苯并环辛炔（ADIBO-F）。氟18取代基是由其甲苯磺酸盐前体制成的，在30分钟的合成时间内以21-35％的放射化学收率分离。ADIBO-F已通过菌株促进的炔-叠氮化物环加成反应，以高放射化学收率和纯度纳入了叠氮化物功能化的，靶向癌症的多肽。最终产品是新型的基于肽的正电子发射断层显像（PET）成像剂，对靶标具有高亲和力，生长激素促分泌素受体1a（GHSR-1a）和胃泌素释放肽受体（GRPR），IC ₅₀值为9.7和0.50 n m， 分别。这是将氟18掺入用于PET成像的生物分子中的新的快速标记选项。