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Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes

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  • Qunchao Zhao

    (National Institutes of Health)

  • Sanjay Telu

    (National Institutes of Health)

  • Shuiyu Lu

    (National Institutes of Health)

  • Victor W. Pike

    (National Institutes of Health)

Abstract

Positron emission tomography (PET) is an advanced biomedical imaging modality that relies on well-designed radiotracers to report on specific protein targets and processes occurring in living animals and humans. Cyclotron-produced short-lived fluorine-18 (t1/2 = 109.8 min) is widely used to radiolabel tracers for PET. Herein we aim to expand the chemical space available for PET tracer development to include structures with 18F-labeled α,α-difluoromethylalkyl groups. We report an efficient and broad-scope method for labeling such groups with high molar activities based on a single-step radiofluorination of α-bromo-α-fluoroalkanes. The method is applicable to bioactive compounds and drug-like molecules, and is readily automated for radiotracer production. The unique physical and biochemical features of the α,α-difluoromethyl group can now be exploited in the design of new PET tracers.

Suggested Citation

  • Qunchao Zhao & Sanjay Telu & Shuiyu Lu & Victor W. Pike, 2025. "Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes," Nature Communications, Nature, vol. 16(1), pages 1-10, December.
    • Handle: RePEc:nat:natcom:v:16:y:2025:i:1:d:10.1038_s41467-025-56897-5
    DOI: 10.1038/s41467-025-56897-5
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