A rapid microfluidic synthesis of [18F]fluoroarenes from nitroarenes

Microfluidic radiofluorodenitrations have been successfully performed using a commercially available microfluidic synthesis system. Reactions of nitroarenes with para-substituted electron withdrawing groups provide incorporation yields ranging from 43 to 97%. Ortho- and meta-substituted nitroarenes provided incorporation yields up to 35%. The reactions were conducted using dry, no-carrier-added [18F]-fluoride and K2CO3/K222 dissolved in N,N-dimethylformamide or dimethyl sulfoxide with total synthesis times of less than five min. The methodology developed in these studies can be applied to the synthesis of a variety of fluorine-18 labeled radiotracers and radiolabeled prosthetic groups from nitroarene precursors.

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► We have used a commercial microfluidic synthesis system to optimize fluorodenitration reactions.
► The optimized reactions are models for many common radiotracers or radiotracer precursors.
► Para-substituted nitroarenes gave radiochemical yields between 40% and 97%.
► Ortho-and meta-substituted nitroarenes gave radiochemical yields up to 35%.