Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics

Science. 2005 Dec 16;310(5755):1793-6. doi: 10.1126/science.1118919.

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-[18F]fluoro-D-glucose ([18F]FDG), in an integrated microfluidic device. Five sequential processes-[18F]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 [18F]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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Automation
  • Fluorides
  • Fluorodeoxyglucose F18 / chemical synthesis*
  • Gas Chromatography-Mass Spectrometry
  • Mice
  • Microfluidics*
  • Miniaturization
  • Molecular Probes / chemical synthesis*
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Rhabdomyosarcoma / diagnostic imaging
  • Solvents
  • Tomography, Emission-Computed

Substances

  • Molecular Probes
  • Radiopharmaceuticals
  • Solvents
  • Fluorodeoxyglucose F18
  • Fluorides