SYNTHESIS OF [F-18]NNC-12-0817 AND [F-18]NNC-12-0818 - 2 POTENTIAL RADIOLIGANDS FOR THE DOPAMINE TRANSPORTER

The preparation of no-carrier-added F-18 labelled NNC 12-0817 oxy]ethy l)-4-[4-oxo-4-(2-thienyl)butyl]piperazine) and NNC 12-0818 ethyl)-4-[4 -hydroxy-4-(2-thienyl)butyl]piperazine) is described. NNC 12-0818 is t he designation of the racemic mixture of two enantiomers. Fluorine-18 is introduced into 4-[F-18]fluoro-4'-fluorobenzophenone from the corre sponding triflate salt by a nucleophilic aromatic substitution reactio n. A no-carrier-added synthesis was performed in 6 steps starting from N,N-dimethylaniline and 4-fluorobenzoyl chloride giving [F-18]NNC 12- 0817 and [F-18]NNC 12-0818 in good yields and a radiochemical purity a fter HPLC-purification higher than 99%.