Huiban Mickael, Pampols-Maso Sabina, Passchier Jan
GlaxoSmithKline, Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, London, UK.
Appl Radiat Isot. 2011 Oct;69(10):1390-4. doi: 10.1016/j.apradiso.2011.05.007. Epub 2011 May 18.
A fully automated and GMP compatible synthesis has been developed to reliably label the M₁ receptor agonist GSK1034702 with carbon-11. Stille reaction of the trimethylstannyl precursor with [¹¹C]methyl iodide afforded [¹¹C]GSK1034702 in an estimated 10 ± 3% decay corrected yield. This method utilises the commercially available modular laboratory equipment and provides high purity [¹¹C]GSK1034702 in a formulation suitable for human use.
已开发出一种完全自动化且符合药品生产质量管理规范（GMP）的合成方法，用于可靠地用碳-11标记M₁受体激动剂GSK1034702。三甲基锡前体与[¹¹C]甲基碘的Stille反应以估计10±3%的衰变校正产率得到[¹¹C]GSK1034702。该方法使用市售的模块化实验室设备，并提供适合人类使用剂型的高纯度[¹¹C]GSK1034702。
