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An efficient synthesis of dopamine transporter tracer [18F]FECNT

机译:多巴胺转运蛋白示踪剂[18F] FECNT的有效合成

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摘要

A simple synthesis of the dopamine transporter ligand [18F]FECNT with high radiochemical yield and short synthesis time, suitable for routine production is reported. Reaction of 2p-carbomethoxy-3P-(4-chlorophenyl)nortropane with [18F]2-fluoroethyl triflate ([18F]FEtOTf) at room temperature for 4 min provided [18F]FECNT in 84% decay corrected radiochemical yield. Since [18F]FEtOTf was prepared from [18F]2-fluoroethyl bromide that was isolated from its starting material, formation of unwanted side products and the amount of expensive precursor used could be greatly reduced. The overall radiochemical yields of [18F]FECNT were 40% (n=29) and the total synthesis time was ca. 100 min. The average specific activity of [18F]FECNT was 377.4 GBq/umol (10.2 Cimol).
机译:报道了一种简单的多巴胺转运体配体[18F] FECNT的合成方法,该方法具有较高的放射化学收率和较短的合成时间,适合常规生产。 2p-羰甲氧基-3P-(4-氯苯基)降冰片烷与[18F] 2-氟乙基三氟甲磺酸酯([18F] FEtOTf)在室温下反应4分钟,可提供[18F] FECNT,其衰变校正后的放射化学产率为84%。由于[18F] FEtOTf是由从其起始原料中分离出的[18F] 2-氟乙基溴制备的,因此可以大大减少不需要的副产物的形成和昂贵的前体的用量。 [18F] FECNT的总放射化学产率为40%(n = 29),总合成时间为。 100分钟[18F] FECNT的平均比活性为377.4 GBq / umol(10.2 Ci / nmol)。

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