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<p>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 (<i>t</i><sub>1/2</sub> = 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 <sup>18</sup>F-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.</p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年2月13日

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  • Qunchao Zhao,
  • Sanjay Telu,
  • Shuiyu Lu,
  • Victor W. Pike

摘要

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.