Help Privacy Policy Disclaimer
  Advanced SearchBrowse




Journal Article

A Transmetalation Reaction Enables the Synthesis of [18F]5-Fluorouracil from [18F]Fluoride for Human PET Imaging

There are no MPG-Authors in the publication available
External Resource
No external resources are shared
Fulltext (restricted access)
There are currently no full texts shared for your IP range.
Fulltext (public)
There are no public fulltexts stored in PuRe
Supplementary Material (public)
There is no public supplementary material available

Hoover, A. J., Lazari, M., Ren, H., Narayanam, M. K., Murphy, J. M., van Dam, R. M., et al. (2016). A Transmetalation Reaction Enables the Synthesis of [18F]5-Fluorouracil from [18F]Fluoride for Human PET Imaging. Organometallics, 35(7), 1008-1014. doi:10.1021/acs.organomet.6b00059.

Cite as: https://hdl.handle.net/11858/00-001M-0000-002B-617A-E
Translation of new F-18-fluorination reactions to produce radiotracers for human positron emission tomography (PET) imaging is rare because the chemistry must have useful scope and the process for F-18-labeled tracer production must be robust and simple to execute. The application of transition metal mediators has enabled impactful F-18-fluorination methods, but to date none of these reactions have been applied to produce a human-injectable PET tracer. In this article we present chemistry and process innovations that culminate in the first production from [F-18]fluoride of human doses of [F-18]5-fluorouracil, a PET tracer for cancer imaging in humans. The first preparation of nickel 6-aryl complexes by transmetalation from arylboronic acids or esters was developed and enabled the synthesis of the [F-18]5-fluorouracil precursor. Routine production of >10 mCi doses of [F-18]5-fluorouracil was accomplished with a new instrument for azeotrope-free [F-18]fluoride concentration in a process that leverages the tolerance of water in nickel-mediated F-18-fluorination.