Fluorine-18 labeling by click chemistry: Multiple probes in one pot

Click chemistry has been widely applied in drug development including radiopharmaceuticals and has shown great advantages. Here we reported a novel strategy for rapid preparation of multiple 18F labeled PET probes in one pot using the ‘Click Reaction’ of Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition of terminal alkynes and organic azides (CuAAC). Preliminary results showed its high efficiency and potential for speeding up the preclinical screening of PET probes.

► With click labeling method, multiple PET probes can be labeled in one pot with high efficiency. ► Under proper HPLC conditions, multiple probes can be separated with high radiochemical purities and chemical purities. ► This strategy if combined with high throughout screening, the discovery of PET probes may be accelerated.