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Copper(I)-free syntheses of [11C/18F]trifluoromethyl ketones from alkyl or aryl esters and [11C/18F]fluoroform
Chemical Communications ( IF 4.9 ) Pub Date : 2024-03-28 , DOI: 10.1039/d4cc00465e
Susovan Jana 1 , Sanjay Telu 1 , Jimmy E. Jakobsson 1 , Bo Yeun Yang 1 , Victor W. Pike 1
Affiliation  

Herein, we report a copper(I)-free method for labeling the trifluoroacetyl group with positron-emitting carbon-11 (t1/2 = 20.4 min) or fluorine-18 (t1/2 = 109.8 min) as part of our exploration of radiolabeled fluoroforms to access new radiolabeled chemotypes of interest for tracer development. Treatment of alkyl esters and aryl esters, containing electron-donating or electron-withdrawing groups, with [11C/18F]fluoroform in the presence of strong base, gave [11C/18F]trifluoromethyl ketones as novel radiolabeling synthons in moderate to high yields within 15 minutes.

中文翻译:

由烷基酯或芳基酯和[11C/18F]氟仿无铜(I)合成[11C/18F]三氟甲基酮

在此,我们报告了一种无铜(I )的方法,用正电子发射碳 11( t 1/2 = 20.4 分钟)或氟 18(t 1/2 = 109.8 分钟)标记三氟乙酰基,作为我们研究的一部分探索放射性标记氟仿,以获得用于示踪剂开发的新放射性标记化学型。在强碱存在下,用[ 11 C/ 18 F]氟仿处理含有给电子或吸电子基团的烷基酯和芳基酯,得到[ 11 C/ 18 F]三氟甲基酮,作为新型放射性标记合成子。 15分钟内达到高产量。
更新日期:2024-03-28
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