Work

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

Year: 2025

Type: article

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 (t 1/2 = 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.

Source: Nature Communications

DOI: 10.1038/s41467-025-56897-5

Authors: Qunchao Zhao, Sanjay Telu, Shuiyu Lu, Victor W. Pike

Institutions: National Institutes of Health, National Institute of Mental Health

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

Open Access status: gold

Estimated APC paid: $6,990

Funders: U.S. Department of Health and Human Services, National Institutes of Health, National Institute of Mental Health, NIH Clinical Center