作为亲电氟化剂的n.c.a. [18F]FClO3的合成研究。

Investigations to the synthesis of n.c.a. [18F]FClO3 as electrophilic fluorinating agent.

作者信息

Hiller A, Fischer C, Jordanova A, Patt J T, Steinbach J

机构信息

Institute of Interdisciplinary Isotope Research, Permoserstrasse 15, D-04318 Leipzig, Germany.

出版信息

Appl Radiat Isot. 2008 Feb;66(2):152-7. doi: 10.1016/j.apradiso.2007.08.016. Epub 2007 Sep 6.

DOI:10.1016/j.apradiso.2007.08.016

PMID:17919916

Abstract

An approach to synthesize the electrophilic fluorinating agent no-carrier-added (n.c.a.) [18F]perchloryl fluoride ([18F]FClO3) in superacidic media in the presence of KClO4 or anhydrous perchloric acid starting from [18F]fluoride was demonstrated in this study. However, the radiochemical yields were low (1-6%) and poorly reproducible. Fluorosulphonic acid proved to be an essential intermediate as revealed by non-radioactive experiments. A key problem in the preparation of [18F]FClO3 is the assumed kinetic inhibition due to the unfavourable stoichiometric ratio of the ClO4 moiety to [18F]HSO3F.

摘要

本研究展示了一种在超酸性介质中，以[¹⁸F]氟化物为起始原料，在高氯酸钾（KClO₄）或无水高氯酸存在的情况下，合成无载体添加（n.c.a.）的亲电氟化剂[¹⁸F]高氯酰氟（[¹⁸F]FClO₃）的方法。然而，其放射化学产率较低（1 - 6%）且重现性差。非放射性实验表明，氟磺酸是必不可少的中间体。制备[¹⁸F]FClO₃的一个关键问题是，由于ClO₄部分与[¹⁸F]HSO₃F的化学计量比不利，推测存在动力学抑制作用。