[¹¹C]CO 与末端炔烃的碳-11 羧化反应。
Carbon-11 carboxylation of terminal alkynes with [ C]CO.
机构信息
Research and Development Department, SYNBIOLAB, Baie-Mahault, Guadeloupe.
Research and Development Department, PMB Head Office, Peynier, France.
出版信息
J Labelled Comp Radiopharm. 2021 May 30;64(6):237-242. doi: 10.1002/jlcr.3907. Epub 2021 Mar 17.
A copper-catalysed radiosynthesis of carbon-11 radiolabelled carboxylic acids was developed by reacting terminal alkynes and cyclotron-produced carbon-11 carbon dioxide ([ C]CO ) in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). A small library of C-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%.
开发了一种铜催化的[¹¹C]标记羧酸的放射性合成方法，通过在 1,8-二氮杂二环[5.4.0]十一碳-7-烯（DBU）的存在下，使末端炔烃和回旋加速器产生的[¹¹C]二氧化碳（[¹¹C]CO）反应。从放射性化学产率为 7%至 28%的末端爆炸（EOB）开始，仅需 15 分钟的总合成时间，就可以得到一个包含 ¹¹C 标记的丙炔酸衍生物的小型文库。
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