Carbon‐11 carboxylation of terminal alkynes with [11C]CO2,Journal of Labelled Compounds and Radiopharmaceuticals

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Carbon‐11 carboxylation of terminal alkynes with [11C]CO2
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2021-03-04 , DOI: 10.1002/jlcr.3907
Francesca Goudou _{1,

2,

3} , Antony D Gee ₃ , Salvatore Bongarzone ₃

Affiliation

A copper‐catalysed radiosynthesis of carbon‐11 radiolabelled carboxylic acids was developed by reacting terminal alkynes and cyclotron‐produced carbon‐11 carbon dioxide ([¹¹C]CO₂) in the presence of 1,8‐diazabicyclo[5.4.0]undec‐7‐ene (DBU). A small library of ¹¹C‐labelled propiolic acid derivatives were obtained with a total synthesis time of 15 min from end of bombardment (EOB) with a (non‐isolated) radiochemical yield ranging from 7% to 28%.

中文翻译：

[11C]CO2 末端炔烃的碳 11 羧化

通过在 1,8-二氮杂双环[5.4.0]undec存在下，末端炔烃与回旋加速器产生的碳-11二氧化碳（[ ¹¹ C]CO ₂ ）反应，开发了铜催化放射合成碳-11放射性标记的羧酸。 ‐7-烯（DBU）。从轰击结束 (EOB) 起，总合成时间为 15 分钟，获得了¹¹ C 标记的丙炔酸衍生物的小型文库，（非分离的）放射化学产率范围为 7% 至 28%。

更新日期：2021-05-04

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