Ascertaining the Suitability of Aryl Sulfonyl Fluorides for [18F]Radiochemistry Applications: A Systematic Investigation using Microfluidics

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• 作者：Lidia Matesic ; Naomi A. Wyatt ; Benjamin H. Fraser ; Maxine P. Roberts ; Tien Q. Pham ; Ivan Greguric
• 刊名：Journal of Organic Chemistry
• 出版年：2013
• 出版时间：November 15, 2013
• 年：2013
• 卷：78
• 期：22
• 页码：11262-11270
• 全文大小：408K
• 年卷期：v.78,no.22(November 15, 2013)
• ISSN：1520-6904

文摘

Optimization of [¹⁸F]radiolabeling conditions and subsequent stability analysis in mobile phase, PBS buffer, and rat serum of 12 aryl sulfonyl chloride precursors with various substituents (electron-withdrawing groups, electron-donating groups, increased steric bulk, heterocyclic) were performed using an Advion NanoTek Microfluidic Synthesis System. A comparison of radiochemical yields and reaction times for a microfluidics device versus a conventional reaction vessel is reported. [¹⁸F]Radiolabeling of sulfonyl chlorides in the presence of competing nucleophiles, H-bond donors, and water was also assessed and demonstrated the versatility and potential utility of [¹⁸F]sulfonyl fluorides as synthons for indirect radiolabeling.