Published in

American Association for the Advancement of Science, Science, 5755(310), p. 1793-1796, 2005

DOI: 10.1126/science.1118919

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Multistep Synthesis of a Radiolabeled Imaging Probe Using Integrated Microfluidics

This paper is available in a repository.
This paper is available in a repository.

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Abstract

Microreactor technology has shown potential for optimizing synthetic efficiency, particularly in preparing sensitive compounds. We achieved the synthesis of an [ 18 F]fluoride-radiolabeled molecular imaging probe, 2-deoxy-2-[ 18 F]fluoro- d -glucose ([ 18 F]FDG), in an integrated microfluidic device. Five sequential processes—[ 18 F]fluoride concentration, water evaporation, radiofluorination, solvent exchange, and hydrolytic deprotection—proceeded with high radio-chemical yield and purity and with shorter synthesis time relative to conventional automated synthesis. Multiple doses of [ 18 F]FDG for positron emission tomography imaging studies in mice were prepared. These results, which constitute a proof of principle for automated multistep syntheses at the nanogram to microgram scale, could be generalized to a range of radiolabeled substrates.