A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids

Pu Zhang; Rongqiang Zhuang; Zhide Guo; Xinhui Su; Xiaoyuan Chen; Xianzhong Zhang

doi:10.1002/chem.201604105

A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids

Chemistry. 2016 Nov 14;22(47):16783-16786. doi: 10.1002/chem.201604105. Epub 2016 Oct 12.

Authors

Pu Zhang¹, Rongqiang Zhuang¹, Zhide Guo¹, Xinhui Su², Xiaoyuan Chen³, Xianzhong Zhang¹

Affiliations

¹ Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen, 361102, P. R. China.
² Zhongshan Hospital Affiliated of Xiamen University, Xiamen, 361004, P. R. China.
³ Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (USA), Bethesda, Maryland, 20892, USA.

PMID: 27730680
DOI: 10.1002/chem.201604105

Abstract

A convenient and quantitative radioiodination method by copper-mediated cross-coupling of aryl boronic acids was developed. The mild labeling conditions, ready availability of the boronic acid substrate, simple operation, broad functional group tolerance and excellent radiochemical yield (RCY) make this a practical strategy for radioiodine labeling without further purification.

Keywords: copper catalysts; molecular imaging; radiochemistry; radioiodination; radiopharmaceuticals.