Synthesis of C-11-labelled acamprosate for PET studies

A method for labelling acamprosate (calcium N-acetyl homotaurinate), an ant i-craving compound For ethanol, with C-11. has been developed for in vivo s tudies 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 u sed 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/m u mol). For the identification of C-11-radioactivity and determination of s pecific radioactivities, HPLC and H-1-NMR were used, Copyright (C), 2001 Jo hn Wiley & Sons. Ltd.