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Tetrabutylammonium tosylate as inert phase-transfer catalyst: The key to high efficiency SN2 radiofluorinations.
Applied Radiation and Isotopes ( IF 1.6 ) Pub Date : 2020-05-19 , DOI: 10.1016/j.apradiso.2020.109195
Viktoriya Orlovskaya 1 , Dmitrii Antuganov 2 , Olga Fedorova 1 , Vasilii Timofeev 3 , Raisa Krasikova 1
Affiliation  

Here we describe use of the tetrabutylammonium p-toluenesulfonate (TBAOTs) as an inert phase transfer catalyst allowing high efficient aliphatic radiofluorination of labeling precursors for the preparation of common radiotracers using only 0.2–1.2 mg of the substrates. With operational convenience (no need for azeotropic drying) and compatibility with the common types of strong anion-exchange cartridges (QMA), this method has a high potential for routine application in various automated synthesizers and offers significant costs reductions due to less precursors used.



中文翻译:

甲苯磺酸四丁铵作为惰性相转移催化剂:高效SN2氟化的关键。

在这里,我们描述了甲苯磺酸四丁基铵(TBAOTs)作为惰性相转移催化剂的使用,它允许仅使用0.2–1.2 mg的底物即可高效地对标记前体进行脂肪族放射性氟化,以制备常见的放射性示踪剂。该方法具有操作便利性(无需共沸干燥)并且与常见类型的强阴离子交换柱(QMA)兼容,因此在各种自动化合成器中具有常规应用的巨大潜力,并且由于使用的前驱物较少,因此可显着降低成本。

更新日期:2020-05-19
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