Radiosynthesis of novel N -18 F-labeled 18 F-FHex-α-l -Glu and 18 F-FHex-β-Glu,Journal of Labelled Compounds and Radiopharmaceuticals

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Radiosynthesis of novel N -18 F-labeled 18 F-FHex-α-l -Glu and 18 F-FHex-β-Glu
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-03-30 , DOI: 10.1002/jlcr.3834
Fuhua Wen _{1,

2} , Shaoyu Liu _{1,

2,

3} , Hui Ma _{1,

2} , Ganghua Tang _{1,

2,

4}

Affiliation

N-18 F-labeled amino acids are important substitutes for new positron emission tomography (PET) imaging tracers complementing the deficiency of 18 F-fluorodeoxyglucose (18 F-FDG). In this work, two novel N-6-18 F-alkyl amino acid imaging agents, 18 F-FHex-α-l-Glu and 18 F-FHex-β-Glu, were designed and synthesized as potential probes for PET imaging of tumors. 18 F-FHex-α-l-Glu was synthesized using the precursor 6 from 18 F-F- with the yield of 16 ± 4% (n = 5, uncorrected) within about 50 minutes. The specific activity was 14.5 GBq/μmol, and the radiochemical purity was more than 95%. 18 F-FHex-β-Glu was synthesized using the precursor 12 based on 18 F-F- with the yield of 11 ± 3% (n = 3, uncorrected) in about 60 minutes. The specific activity was 9.1 GBq/μmol, and the radiochemical purity was more than 95%.

中文翻译：

新型 N -18 F 标记的 18 F-FHex-α-l -Glu 和 18 F-FHex-β-Glu 的放射合成

N-18 F 标记的氨基酸是新正电子发射断层扫描 (PET) 成像示踪剂的重要替代品，可补充 18 F-氟脱氧葡萄糖 (18 F-FDG) 的不足。在这项工作中，设计并合成了两种新型 N-6-18 F-烷基氨基酸显像剂 18 F-FHex-α-l-Glu 和 18 F-FHex-β-Glu 作为 PET 成像的潜在探针。肿瘤。使用来自 18 FF-的前体 6 合成 18 F-FHex-α-l-Glu，在约 50 分钟内以 16 ± 4%（n = 5，未校正）的产率合成。比活为14.5 GBq/μmol，放化纯度大于95%。18 F-FHex-β-Glu 是使用基于 18 FF-的前体 12 在大约 60 分钟内以 11 ± 3%（n = 3，未校正）的产率合成的。比活为9.1 GBq/μmol，放化纯度大于95%。

更新日期：2020-03-30

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