Morgan, T. E.F., Riley, L. M., Tavares, A. A.S. and Sutherland, A. (2021) Automated Radiosynthesis of cis- and trans-4-[18F]Fluoro-L-proline using [18F]Fluoride. Journal of Organic Chemistry, 86(20), pp. 14054-14060. (doi: 10.1021/acs.joc.1c00755) (PMID:33913318) (PMCID:PMC8524414)
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Abstract
The positron emission tomography imaging agents cis- and trans-4-[18F]fluoro-l-proline are used for the detection of numerous diseases such as pulmonary fibrosis and various carcinomas. These imaging agents are typically prepared by nucleophilic fluorination of 4-hydroxy-l-proline derivatives, with [18F]fluoride, followed by deprotection. Although effective radiofluorination reactions have been developed, the overall radiosynthesis process is suboptimal due to deprotection methods that are performed manually, require multiple steps, or involve harsh conditions. Here we describe the development of two synthetic routes that allow access to precursors, which undergo highly selective radiofluorination reactions and rapid deprotection, under mild acidic conditions. These methods were found to be compatible with automation, avoiding manual handling of radioactive intermediates.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Riley, Miss Leanne and Sutherland, Professor Andrew |
| Authors: | Morgan, T. E.F., Riley, L. M., Tavares, A. A.S., and Sutherland, A. |
| College/School: | College of Science and Engineering > School of Chemistry |
| Journal Name: | Journal of Organic Chemistry |
| Publisher: | American Chemical Society |
| ISSN: | 0022-3263 |
| ISSN (Online): | 1520-6904 |
| Published Online: | 29 April 2021 |
| Copyright Holders: | Copyright © 2021 The Authors |
| First Published: | First published in Journal of Organic Chemistry 86(20): 14054-14060 |
| Publisher Policy: | Reproduced under a Creative Commons licence |
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