Synthesis of 11C-labelled acamprosate for PET studies

A method for labelling acamprosate (calcium N-acetyl homotaurinate), an anti-craving compound For ethanol, with C-11. has been developed for in vivo studies with positron emission tomography (PET). The synthesis was based on the acylation of homotaurinate using [C-11]acetyl chloride as the labelling agent. Reversed-phase HPLC in highly aqueous mobile phase conditions was used for product purification. The radiochemical yield achieved was about 1.14 GBq (31 mCi) with a specific radioactivity of 8.14 GBq/mu mol (220 mCi/mu mol). For the identification of C-11-radioactivity and determination of specific radioactivities, HPLC and H-1-NMR were used, Copyright (C), 2001 John Wiley & Sons. Ltd.