Sequential Radiosynthetic Methodology: Assembly of Boronic Ester Precursors on a Diol Resin and Radioiodination Using Copper-Mediated Radioiododeboronation and Azide–Alkyne Cycloaddition
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.
Authors
- Hiroyuki Yasui (ORCID: https://orcid.org/0000-0003-3317-3947)
- Hidekazu Kawashima (ORCID: https://orcid.org/0000-0003-4078-4199)
- Yuto Kondo (ORCID: https://orcid.org/0000-0003-3529-9703)
- Kazuhiro Takahashi (ORCID: https://orcid.org/0000-0001-8943-1875)
- Hiroyuki Kimura (ORCID: https://orcid.org/0000-0002-4291-3524)
- Yasunao Hattori
- Mamiko Tanaka
Institutions
- Kanazawa University (JP)
- Fukushima Medical University (JP)
- Kyoto Pharmaceutical University (JP)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-06-09
- DOI
- https://doi.org/10.1021/acs.joc.5c00382
- Primary Topic
- Radiopharmaceutical Chemistry and Applications
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Japan Society for the Promotion of Science