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Published May 28, 2008 | Supplemental Material
Journal Article Open

Synthesis of Fluorine-18 Functionalized Nanoparticles for use as in vivo Molecular Imaging Agents


Nanoparticles containing fluorine-18 were prepared from block copolymers made by ring opening metathesis polymerization (ROMP). Using the fast initiating ruthenium metathesis catalyst (H_2IMes)(pyr)_2(Cl)_2Ru=CHPh, low polydispersity amphiphilic block copolymers were prepared from a cinnamoyl-containing hydrophobic norbornene monomer and a mesyl-terminated PEG-containing hydrophilic norbornene monomer. Self-assembly into micelles and subsequent cross-linking of the micelle cores by light-activated dimerization of the cinnamoyl groups yielded stable nanoparticles. Incorporation of fluorine-18 was achieved by nucleophilic displacement of the mesylates by the radioactive fluoride ion with 31% incorporation of radioactivity. The resulting positron-emitting nanoparticles are to be used as in vivo molecular imaging agents for use in tumor imaging.

Additional Information

© 2008 American Chemical Society. Received March 18, 2008. Publication Date (Web): May 2, 2008. Published In Issue May 28, 2008. We acknowledge the National Cancer Institute (grant No. 5U54 CA119347) and the National Science Foundation (grant No. CHE-0410425) for support of this research. We would also like to thank Peigen Cao and Jim Heath for help with the AFM images and size distribution measurements, Mark Davis for assistance with DLS measurements, and Nagichettiar Satyamurthy for help and advice with the radiolabeling experiments. Supporting Information: Experimental procedures, characterization data, AFM images, and radioTLC. This material is available free of charge via the Internet at http://pubs.acs.org.

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