New approach for the synthesis of [ 18F]fluoroethyltyrosine for cancer imaging: Simple, fast, and high yielding automated synthesis

Abstract

O-(2-[ 18F]fluoroethyl)- l-tyrosine ([ 18F]FET) is one of the first 18F-labeled amino acids for imaging amino acid metabolism in tumors. This tracer overcomes the disadvantages of [ 18F]fluorodeoxyglucose, [ 18F]FDG, and [ 11C]methionine, [ 11C]MET. Nevertheless, the various synthetic methods providing 18F[FET] exhibit a big disadvantage concerning the necessity of two purification steps during the synthesis including HPLC purification, which causes difficulties in the automation, moderate yields, and long synthesis times >60 min. A new approach for the synthesis of [ 18F]FET is developed starting from 2-bromoethyl triflate as precursor. After optimization of the synthesis parameters including the distillation step of [ 18F]-FCH 2CH 2Br combined with the final purification of [ 18F]FET using a simple solid phase extraction instead of an HPLC run the synthesis [ 18F]FET could be significantly simplified, shortened, and improved. The radiochemical yield (RCY) was about 45% (not decay corrected and calculated relative to [ 18F]F − activity that was delivered from the cyclotron). Synthesis time was only 35 min from the end of bombardment (EOB) and the radiochemical purity was >99% at the end of synthesis (EOS). Thus, this simplified synthesis for [ 18F]FET offers a very good option for routine clinical use.