Abstract
High reactivity of [11C]-methyl iodide ([11C]CH3I) with the thiol group was demonstrated with cysteamine and other compounds containing a thiol and another functional groups in each structure. The methylation of the thiol group in cysteamine with [11C]CH3I was very rapid at 0°C with no catalyst, and gave a high radiochemical yield and purity without any detectable by-product. Moreover, this reaction was not disturbed by the other functional groups, such as -NH2, -OH and -COOH in the same structure. This S-methylation reaction is very useful for producing a new radiopharmaceutical labeled with the short lived positron emitting nuclide C-11.
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Magata, Y., Saji, H., Tokui, T. et al. High reactivity of [11C]CH3I with thiol group in the synthesis of C-11 labeled radiopharmaceuticals. Ann Nucl Med 7, 173–177 (1993). https://doi.org/10.1007/BF03164962
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DOI: https://doi.org/10.1007/BF03164962