Increasing attention has been focused on synthesis radiopharmaceuticals for positron emission tomography (PET). The recent years witnessed applications of click chemistry to PET radiopharmaceutical synthesis

because of its distinctive advantages including high speed

yield and stereospecificity under mild conditions. Synthesis of 18F-labeled and 11C-labeled radiopharmaceuticals and intermediates via click chemistry are reviewed. The future trend of click chemistry for the synthesis of PET radiopharmaceutical is prospected.