A streamlined radiosynthetic methodology enables the precise sequential assembly of boronic ester precursors on diol resin, seamlessly integrating copper-mediated radioiododeboronation and azide-alkyne cycloaddition. This approach yields radioiodinated compounds with high radiochemical conversion (>90%) without requiring column purification until the final stage, thereby accelerating the efficient development of advanced radioiodinated molecular probes.
The Journal of organic chemistry. 2025 Jun 9. doi: 10.1021/acs.joc.5c00382
Sequential Radiosynthetic Methodology: Assembly of Boronic Ester Precursors on a Diol Resin and Radioiodination Using Copper-Mediated Radioiododeboronation and Azide-Alkyne Cycloaddition
序贯放射合成法:在二醇树脂上装配硼酸酯前体,并通过铜介导的放射性碘脱硼化和叠氮-炔环加成进行放射性碘标记 翻译改进
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DOI: 10.1021/acs.joc.5c00382 PMID: 40490409
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