从[C]羰基化合物到[C]酰胺：通过光延反应的快速一锅法合成。

Bongarzone S, Runser A, Taddei C, Dheere A K Haji, Gee A D

Division of Imaging Sciences and Biomedical Engineering, King's College London, King's Health Partners, St. Thomas' Hospital, London, SE1 7EH, UK.

Chem Commun (Camb). 2017 May 9;53(38):5334-5337. doi: 10.1039/c7cc01407d.

A novel amide synthesis methodology is described using amines, CO and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [C]CO. The synthetic utility of the one-pot labelling methodology was demonstrated by producing [C]melatonin. The incorporation of [C]CO into [C]melatonin was 36% - determined by radioHPLC 2 min post [C]CO delivery.

描述了一种使用胺、一氧化碳和格氏试剂以及光延试剂的新型酰胺合成方法。该方法应用于碳-11放射化学，使用回旋加速器产生的[¹¹C]CO标记酰胺。通过制备[¹¹C]褪黑素证明了一锅法标记方法的合成实用性。在[¹¹C]CO递送后2分钟通过放射性高效液相色谱法测定，[¹¹C]CO掺入[¹¹C]褪黑素的比例为36%。