This report describes a method for the nucleophilic radiofluorination of (hetero)aryl chlorides, (hetero)aryl triflates, and nitroarenes using a combination of [F]KF·K and MeNHCO for the in situ formation of a strongly nucleophilic fluorinating reagent (proposed to be [F]MeNF). This method is applied to 24 substrates bearing diverse functional groups, and it generates [F](hetero)aryl fluoride products in good to excellent radiochemical yields in the presence of ambient air/moisture. The reaction is applied to the preparation of F-labeled HQ-415 for potential (pre)clinical use.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8826450 | PMC |
| http://dx.doi.org/10.1021/acs.joc.1c01491 | DOI Listing |
Publication Analysis
Top Keywords
sar radiofluorination
4
radiofluorination situ
4
situ generated
4
generated [f]tetramethylammonium
4
[f]tetramethylammonium fluoride
4
fluoride report
4
report describes
4
describes method
4
method nucleophilic
4
nucleophilic radiofluorination
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!