Copper-mediated radiofluorination is a straightforward method to produce a variety of [18F]fluoroarenes and [18F]fluoroheteroarenes. To minimize the number of steps in the production of 18F-labelled radiopharmaceuticals, we have developed a short and efficient azeotropic drying-free 18F-labelling method using copper-mediated fluorination. Our goal was to improve the copper-mediated method to achieve wide substrate scope with good radiochemical yields with short synthesis time. Solid phase extraction with Cu (OTf)2 in dimethylacetamide is a suitable activation method for [18F]fluoride. Elution efficiency with Cu (OTf)2 is up to 79% and radiochemical yield (RCY) of a variety of model molecules in the crude reaction mixture has reached over 90%. Clinically relevant molecules, norepinephrine transporter tracer [18F]NS12137 and monoamine transporter tracer [18F]CFT were produced with 16.5% RCY in 98 min and 5.3% RCY in 64 min, respectively. Cu (OTf)2 is a suitable elution agent for releasing [18F]fluoride from an anion exchange cartridge. The method is fast and efficient and the Cu-complex is customizable after the release of [18F]fluoride. Alterations in the [18F]fluoride elution techniques did not have a negative effect on the subsequent labelling reactions. We anticipate this improved [18F]fluoride elution technique to supplant the traditional azeotropic drying of [18F]fluoride in the long run and to concurrently enable the variations of the copper-complex.

中文翻译：

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快速高效的铜介导的18F氟化芳基斯坦酮，芳基硼酸和芳基硼酸酯，无需共沸干燥。

铜介导的放射性氟化是生产各种[18F]氟芳烃和[18F]氟杂芳烃的直接方法。为了最大程度地减少18F标记放射性药物的生产步骤，我们开发了一种使用铜介导的氟化方法的短而有效的无共沸无干燥18F标记方法。我们的目标是改进铜介导的方法，以在短合成时间内以良好的放射化学收率实现较宽的底物范围。用二甲基乙酰胺中的Cu（OTf）2进行固相萃取是[18F]氟化物的合适活化方法。Cu（OTf）2的洗脱效率高达79％，粗反应混合物中多种模型分子的放射化学产率（RCY）已达到90％以上。临床相关分子 去甲肾上腺素转运蛋白示踪剂[18F] NS12137和单胺转运蛋白示踪剂[18F] CFT分别在98分钟和16分钟内产生了16.5％的RCY和在64分钟内产生了5.3％的RCY。Cu（OTf）2是用于从阴离子交换盒释放[18F]氟化物的合适洗脱剂。该方法快速高效，并且在[18F]氟化物释放后可定制铜络合物。[18 F]氟化物洗脱技术的改变对随后的标记反应没有负面影响。我们预计，从长远来看，这种改进的[18F]氟化物洗脱技术将取代[18F]氟化物的传统共沸干燥方法，并同时实现铜配合物的变化。Cu（OTf）2是用于从阴离子交换盒释放[18F]氟化物的合适洗脱剂。该方法快速高效，并且在[18F]氟化物释放后可定制铜络合物。[18 F]氟化物洗脱技术的改变对随后的标记反应没有负面影响。我们预计，从长远来看，这种改进的[18F]氟化物洗脱技术将取代[18F]氟化物的传统共沸干燥方法，并同时实现铜配合物的变化。Cu（OTf）2是用于从阴离子交换盒释放[18F]氟化物的合适洗脱剂。该方法快速高效，并且在[18F]氟化物释放后可定制铜络合物。[18 F]氟化物洗脱技术的改变对随后的标记反应没有负面影响。我们预计，从长远来看，这种改进的[18F]氟化物洗脱技术将取代[18F]氟化物的传统共沸干燥方法，并同时实现铜配合物的变化。