A Novel Reagent for Labeling PET Tracers at Trifluoromethyl Groups

The molecular imaging technique of positron emission tomography (PET) is an increasingly important tool in biomedical research and in drug discovery and development. Many small molecule drugs and potential PET radiotracers carry trifluoromethyl (CF3) groups. Because CF3 groups are generally considered to be metabolically stable, there is a strong interest in developing drugs with these groups. This invention describes a novel method and apparatus for producing no-carrier added [11C]fluoroalkanes, which can be used as labeling agents for PET radiotracers at CF3 groups. Prior to this technology, no method for [11C]fluoroalkyaltion has existed. The reported method, which involves passing [11C]methane over a heated column of a metal fluoride, has high yield and high specificity, is simple, fast, and capable of being fully automated. Of special interest is the efficient production of [11C]fluoroform, which can be readily applied to labeling a variety of chemotypes with a [11C]trifluoromethyl group.

Potential Commercial Applications: Competitive Advantages:
  • Apparatus for producing no-carrier added [11C]fluoroalkanes
  • CF3-based PET labeling agents
  • High yield
  • High molar activity
  • Increased simplicity
  • Capable of automation
  • Rapid method to produce PET radiotracers (~15 min)


Victor Pike (NIMH)  ➽ more inventions...

Mohammad Haskali (NIMH)  ➽ more inventions...

Intellectual Property:
US Pat: - issued -
PCT Application No. PCT/US2017/060838 filed on 2017-11-09
US Application No. 16/349,124 filed on 2019-05-10
US Application No. 17/074,832 filed on 2020-10-20

Haskali MB, Pike VW. PMID 28514059

Collaboration Opportunity:

The National Institute of Mental Health is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize method and labeling agents for PET tracers. For collaboration opportunities, please contact Victor W. Pike, Ph.D. at pikev@mail.nih.gov.

Licensing Contact:
Anton Dawson, Ph.D.
Email: anton.dawson@nih.gov
Phone: 301-496-6784

OTT Reference No: E-259-2016-0
Updated: Jun 28, 2018