Synthesis of No-Carrier-Added 4-[18F]Fluorophenol from 4-Benzyloxyphenyl-(2-thienyl)iodonium Bromide

Molecules

Tobias L. Ross¹  Johannes Ermert¹ 

[1] Institute of Neuroscience and Medicine, INM-5: Nuclear Chemistry, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany ^†Current address: Institute of Nuclear Chemistry, Johannes Gutenberg-University Mainz, 55128 Mainz, Germany.

关键词: fluorine-18;    4-[¹⁸F]fluorophenol;    diaryl iodonium salts;    radiosynthesis;    positron emission tomography;   

DOI  :  10.3390/molecules16097621

来源: mdpi

【 摘 要 】

4-[¹⁸F]Fluorophenol is a versatile synthon for the synthesis of more complex radiopharmaceuticals bearing a 4-[¹⁸F]fluorophenoxy moiety. In order to prepare 4-[¹⁸F]fluorophenol in no-carrier-added (n.c.a.) form only a nucleophilic labelling method starting from [¹⁸F]fluoride is suitable. In this paper a new, two step radiosynthesis starting from 4-benzyloxyphenyl-(2-thienyl)iodonium bromide and [¹⁸F]fluoride with subsequent deprotection is described, yielding n.c.a. [¹⁸F]fluorophenol in 34 to 36% radiochemical yield.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.