Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes
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 t...
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2025-02-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/s41467-025-56897-5 |
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| author | Qunchao Zhao Sanjay Telu Shuiyu Lu Victor W. Pike |
| author_facet | Qunchao Zhao Sanjay Telu Shuiyu Lu Victor W. Pike |
| author_sort | Qunchao Zhao |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-9a860d222626461390c8a068f45e1b77 |
| institution | OA Journals |
| issn | 2041-1723 |
| language | English |
| publishDate | 2025-02-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Nature Communications |
| spelling | doaj-art-9a860d222626461390c8a068f45e1b772025-08-20T02:12:58ZengNature PortfolioNature Communications2041-17232025-02-0116111010.1038/s41467-025-56897-5Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanesQunchao Zhao0Sanjay Telu1Shuiyu Lu2Victor W. Pike3Molecular Imaging Branch, National Institute of Mental Health, National Institutes of HealthMolecular Imaging Branch, National Institute of Mental Health, National Institutes of HealthMolecular Imaging Branch, National Institute of Mental Health, National Institutes of HealthMolecular Imaging Branch, National Institute of Mental Health, National Institutes of HealthAbstract 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.https://doi.org/10.1038/s41467-025-56897-5 |
| spellingShingle | Qunchao Zhao Sanjay Telu Shuiyu Lu Victor W. Pike Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes Nature Communications |
| title | Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes |
| title_full | Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes |
| title_fullStr | Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes |
| title_full_unstemmed | Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes |
| title_short | Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes |
| title_sort | expanding tracer space for positron emission tomography with high molar activity 18f labeled α α difluoromethylalkanes |
| url | https://doi.org/10.1038/s41467-025-56897-5 |
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