Fully automated synthesis of the M₁ receptor agonist [¹¹C]GSK1034702 for clinical use on an Eckert & Ziegler Modular Lab system

Mickael Huiban; Sabina Pampols-Maso; Jan Passchier

doi:10.1016/j.apradiso.2011.05.007

Fully automated synthesis of the M₁ receptor agonist [¹¹C]GSK1034702 for clinical use on an Eckert & Ziegler Modular Lab system

Appl Radiat Isot. 2011 Oct;69(10):1390-4. doi: 10.1016/j.apradiso.2011.05.007. Epub 2011 May 18.

Authors

Mickael Huiban¹, Sabina Pampols-Maso, Jan Passchier

Affiliation

¹ GlaxoSmithKline, Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, London, UK. [email protected]

PMID: 21605979
DOI: 10.1016/j.apradiso.2011.05.007

Abstract

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.

MeSH terms

Automation, Laboratory
Benzimidazoles / chemical synthesis*
Carbon Radioisotopes
Cholinergic Agonists / chemical synthesis*
Isotope Labeling
Radiopharmaceuticals / chemical synthesis*
Receptor, Muscarinic M1 / agonists*

Substances

Benzimidazoles
Carbon Radioisotopes
Cholinergic Agonists
GSK 1034702
Radiopharmaceuticals
Receptor, Muscarinic M1