在“极简主义”条件下，使用铜介导的放射性氟化反应自动合成4-[(18)F]氟代苯甲醚、[(18)F]DAA1106和4-[(18)F]FPhe 。
Automated synthesis of 4-[(18)F]fluoroanisole, [(18)F]DAA1106 and 4-[(18)F]FPhe using Cu-mediated radiofluorination under "minimalist" conditions.
作者信息
Zischler Johannes, Krapf Philipp, Richarz Raphael, Zlatopolskiy Boris D, Neumaier Bernd
机构信息
Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
Institute of Radiochemistry and Experimental Molecular Imaging, University Clinic Cologne, Kerpener Str. 62, 50937 Cologne, Germany; Max Planck Institute for Metabolism Research, Gleueler Str. 50, 50931 Cologne, Germany.
出版信息
Appl Radiat Isot. 2016 Sep;115:133-137. doi: 10.1016/j.apradiso.2016.04.030. Epub 2016 May 27.
The application of the "minimalist" approach to Cu-mediated radiofluorination allows the efficient preparation of (18)F-labeled arenes regardless of their electronic properties. The implementation of this methodology on a commercially available synthesis module (hotbox(three), Scintomics, Germany) enabled the automated production of 4-[(18)F]fluoroanisole as well as the clinically relevant PET-tracers, 4-[(18)F]FPhe and [(18)F]DAA1106, in radiochemical yields of 41-61% and radiochemical purities of >95% within 30-60min. These results demonstrated the high efficacy and versatility of the developed method that will open up opportunities for a broad application of Cu-mediated radiofluorination in PET-chemistry.
将“极简主义”方法应用于铜介导的放射性氟化反应，能够高效制备（18）F标记的芳烃，而无需考虑其电子性质。在市售合成模块（hotbox(three)，德国Scintomics公司）上实施该方法，能够在30 - 60分钟内自动生产4-[(18)F]氟苯甲醚以及具有临床相关性的PET示踪剂4-[(18)F]FPhe和[(18)F]DAA1106，放射化学产率为41 - 61%，放射化学纯度>95%。这些结果证明了所开发方法的高效性和通用性，这将为铜介导的放射性氟化反应在PET化学中的广泛应用开辟机会。
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