Multistep synthesis of a radiolabeled imaging probe using integrated microfluidics.
Lee CC,
Sui G,
Elizarov A,
Shu CJ,
Shin YS,
Dooley AN,
Huang J,
Daridon A,
Wyatt P,
Stout D,
Kolb HC,
Witte ON,
Satyamurthy N,
Heath JR,
Phelps ME,
Quake SR,
Tseng HR.
Department of Bioengineering, California Institute of Technology, Pasadena, CA 91125, USA.
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.
PMID: 16357255 [PubMed - indexed for MEDLINE]