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Rapid One-Step 18F-Labeling of Peptides via Heteroaromatic Silicon-Fluoride Acceptors.
Organic Letters ( IF 5.2 ) Pub Date : 2020-01-13 , DOI: 10.1021/acs.orglett.9b04160
Maruthi Kumar Narayanam 1 , Anton A Toutov 2 , Jennifer M Murphy 1
Affiliation  

A new class of organosilicon-based radiosynthons, heteroaromatic silicon-fluoride acceptors, namely, HetSiFAs, that readily undergo isotope exchange with dry [18F]fluoride at room temperature in high radiochemical yield (up to 94%) with good molar activity is reported. Radiofluorination proceeds in a single step in 2 min without high-performance liquid chromatography purification to provide an operationally simple method for 18F-PET tracer production. This method was used to prepare an 18F-labeled commercial tetrapeptide, and positron emission tomography imaging confirmed in vivo stability.

中文翻译:

通过杂芳族氟化硅受体快速一步一步进行18F肽标记。

据报道,一类新型的有机硅基放射性合成子,即杂芳族氟化硅受体,即HetSiFAs,在室温下易于与干燥的[18F]氟化物进行同位素交换,且放射化学收率高(高达94%),具有良好的摩尔活性。放射性氟化仅需2分钟即可一步完成,而无需进行高效液相色谱纯化,从而为生产18F-PET示踪剂提供了一种操作简单的方法。该方法用于制备18 F标记的市售四肽,正电子发射断层显像证实其体内稳定性。
更新日期:2020-01-13
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