Journal article

Ethyl Pinacol Boronates as Advantageous Precursors for Copper-Mediated Radiofluorination

Abstract:: (Hetero)aryl pinacol boronic esters are routinely used for 18F-labeling and have accelerated numerous diagnostic and drug discovery programs. An analysis of the current state-of-play, however, highlights a pending challenge. Reports have indicated that some pinacol boronic esters are unstable and difficult to purify, hindering broader adoption in the clinic. Herein, we demonstrate that more stable boronic esters derived from 3,4-diethylhexane-3,4-diol (Epin) are highly suitable for copper-mediated radiolabeling. Impact is illustrated with the automated synthesis of [18F]FMZ.

Publication status:: Published

Peer review status:: Peer reviewed

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APA Style

Hadjipaschalis, N., Ortalli, S., Chen, Z., Paton, R. S., Ford, J., Tredwell, M., & Gouverneur, V. (2025). Ethyl Pinacol Boronates as Advantageous Precursors for Copper-Mediated Radiofluorination. Organic Letters, 27(24), 6545–6550.

MLA Style

Hadjipaschalis, N, et al. “Ethyl Pinacol Boronates as Advantageous Precursors for Copper-Mediated Radiofluorination.” Organic Letters, vol. 27, no. 24, 2025, pp. 6545–50.

Chicago Style

Hadjipaschalis, N, S Ortalli, Z Chen, et al. 2025. “Ethyl Pinacol Boronates as Advantageous Precursors for Copper-Mediated Radiofluorination.” Organic Letters 27 (24): 6545–50.
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Files:: Hadjipaschalis_et_al_2025_Ethyl_Pinacol_Boronates.pdf

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Publisher copy:: 10.1021/acs.orglett.5c02055

Authors

+ Hadjipaschalis, N More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ Ortalli, S More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ Chen, Z More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

+ Paton, RS More by this author

Role:: Author
ORCID:: 0000-0002-0104-4166

+ Ford, J More by this author

Institution:: University of Oxford
Division:: MPLS
Department:: Chemistry
Sub department:: Chemistry Research Laboratory
Role:: Author

More authors...

+ Division of Chemistry More from this funder

Funder identifier:: https://ror.org/01ar8dr59

+ Engineering and Physical Sciences Research Council More from this funder

Funder identifier:: https://ror.org/0439y7842

+ Biotechnology and Biological Sciences Research Council More from this funder

Funder identifier:: https://ror.org/00cwqg982

Publisher:: American Chemical Society
Journal:: Organic Letters More from this journal
Volume:: 27
Issue:: 24
Pages:: 6545-6550
Publication date:: 2025-06-10
Acceptance date:: 2025-06-05
DOI:: 10.1021/acs.orglett.5c02055
EISSN:: 1523-7052
ISSN:: 1523-7060

Language:: English
Pubs id:: 2129705
Local pid:: pubs:2129705
Source identifiers:: 3045421
Deposit date:: 2025-06-23
ARK identifier:: ark:/29072/ora_262de4266fc84f69960c1a233112bfca

Terms of use

Copyright date:: 2025

Licence:: CC Attribution (CC BY)

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