A convenient, high-yield synthesis of [18F]4-fluoroantipyrine using [18F]acetylhypofluorite

Mirko Diksic, Pasquale Diraddo
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引用次数: 8

Abstract

This paper describes a convenient, high-yield synthesis of [18F]4-fluoroantipyrine, a blood flow tracer, by fluorination of antipyrine with [18F]acetylhypofluorite prepared in situ. The radiopharmaceutical was obtained in a radiochemical yield of 28 and 30% following HPLC and Sep-Pak purification, respectively. The two different purification procedures of the crude reaction are described. Sep-Pak filtration, after decomposition of the intermediary of the fluorination reaction by heating with NaOCH3 in CH3CN, produced a radiopharmaceutical with radiochemical purity of more than 98%. The synthesis requires 50 min following irradiation.

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用[18F]乙酰次萤石合成[18F]4-氟安替吡林的一种方便、高产率的方法
本文介绍了用原位制备的[18F]乙酰次萤石氟化安替比林,方便、高产地合成血流示踪剂[18F]4-氟安替比林。经高效液相色谱和Sep-Pak纯化,得到的放射性药物的放射化学产率分别为28%和30%。介绍了粗反应的两种不同纯化工艺。Sep-Pak过滤,用NaOCH3在CH3CN中加热分解氟化反应的中间体,制得放射化学纯度大于98%的放射性药物。辐照后需50分钟合成。
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