Radiosynthesis of 3′-deoxy-3′-[18F]fluorothymidine:: [18F]FLT for imaging of cellular proliferation in vivo

A reliable radiosynthesis of 3'-deoxy-3'-[F-18]fluorothymidine ([F-18]FLT) has been developed based on [F-18]fluoride displacement of a protected nosylate precursor. A simple three-step synthesis is described that is useful for preparing >10 mCi (370 MBq) of radiochemically pure [F-18]FLT, with a specific activity >1 Ci/mu mol (37 GBq/mu mol) at EOS within 100 min and in 13% radiochemical yield tend of bombardment (EOB); 7% end of synthesis (EOS). [F-18]FLT has been designed as a new positron emission tomography imaging agent for visualizing cellular proliferation in vivo based on the metabolism of thymidine. NUCL MED BIOL 27;2:143-156, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.