GB2463436A — (11C)methoxy-radiolabelled 2,3',4,5'-tetramethylstilbene (TMS) and its preparation and use

USPTO Abstract

This invention pertains generally to the field of radiochemical synthesis, and more specifically to methods of preparing [11C]methoxy-radiolabelled 2,3',4,5' -tetramethoxystilbene (TMS) from an unlabelled hydroxy precursor of 2,3',4,5' -tetramethoxystilbene (TMS) that has a pendant hydroxyl group, by reaction with [11C]methyl trifluoromethanesulfonate (CF3SO2O11CH3), also known as [11C]methyl triflate, or [11C]methyl iodide (11CH3I). This reaction converts the pendant hydroxyl group into a pendant [11C]methoxy group. The resulting [11C]methoxy-radiolabelled product is useful, for example, as an in vivo positron emission tomography (PET) tracer, for example, for tumours (e.g., cancer tumours) and/or beta amyloid plaques (e.g., Alzheimer's disease). The present invention also pertains to the resulting [11C]methoxy radiolabelled products, compositions comprising them, their use in methods of (e.g., PET) imaging, their use in methods of medical treatment and diagnosis, etc.