Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane
Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane
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DOI：
10.1016/j.tetlet.2003.10.034
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发表时间：
2003-12-15
影响因子：
1.8
通讯作者：
Rösch, F
中科院分区：
文献类型：
--
作者：
Bauman, A;Piel, M;Rösch, F
通过添加碱金属碘化物，可以显著提高使用次级标记前体2-[F-18]氟乙基甲苯磺酸酯（[（18）]FETos）和1-溴-2-[F-18]氟乙烷（[F-18]BFE）的几种化合物的放射化学F-18-氚产率。例如，[F-18]氟乙基胆碱的放射化学产率可以用[F-18]BFE加倍，用[F-18]FETos从13%增加到约80%。通过向前体中加入碱金属碘化物，可以显著提高已建立的放射性药物的F-18-氟乙基化产率，特别是在自动化合成的情况下，而不需要对反应条件进行重大改变。(C)2003 Elsevier Ltd.保留所有权利。
Radiochemical F-18-fluorination yields of several compounds using the secondary labelling precursors 2-[F-18]fluoroethyl tosylate ([(18)]FETos) and 1-bromo-2-[F-18]fluoroethane ([F-18]BFE) could be considerably enhanced by the addition of an alkali iodide. The radiochemical yield of [F-18]fluoroethyl choline for example could be doubled with [F-18]BFE and increased from 13% to approximate to80% with [F-18]FETos. By addition of alkali iodide to the precursor, the F-18-fluoroethylation yields of established radiopharmaceuticals, especially in the case of automated syntheses, could be significantly increased without major changes of the reaction conditions. (C) 2003 Elsevier Ltd. All rights reserved.