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Fast and efficient copper-mediated 18F-fluorination of arylstannanes, aryl boronic acids, and aryl boronic esters without azeotropic drying

Salla Orvokki Lahdenpohja; Johan Rajander; Anna Kaarina Kirjavainen; Noora Annika Rajala

Fast and efficient copper-mediated 18F-fluorination of arylstannanes, aryl boronic acids, and aryl boronic esters without azeotropic drying

Salla Orvokki Lahdenpohja
Johan Rajander
Anna Kaarina Kirjavainen
Noora Annika Rajala
Katso/Avaa
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Springer Internat. Publ.
doi:10.1186/s41181-019-0079-y
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Julkaisun pysyvä osoite on:
https://urn.fi/URN:NBN:fi-fe2021042824648
Tiivistelmä

Background

Copper-mediated radiofluorination is a straightforward method to produce a variety of [18F]fluoroarenes and [18F]fluoroheteroarenes. To minimize the number of steps in the production of 18F-labelled radiopharmaceuticals, we have developed a short and efficient azeotropic drying-free 18F-labelling
method using copper-mediated fluorination. Our goal was to improve the
copper-mediated method to achieve wide substrate scope with good
radiochemical yields with short synthesis time.

Results

Solid phase extraction with Cu (OTf)2 in dimethylacetamide is a suitable activation method for [18F]fluoride. Elution efficiency with Cu (OTf)2
is up to 79% and radiochemical yield (RCY) of a variety of model
molecules in the crude reaction mixture has reached over 90%. Clinically
relevant molecules, norepinephrine transporter tracer [18F]NS12137 and monoamine transporter tracer [18F]CFT were produced with 16.5% RCY in 98 min and 5.3% RCY in 64 min, respectively.

Conclusions

Cu (OTf)2 is a suitable elution agent for releasing [18F]fluoride
from an anion exchange cartridge. The method is fast and efficient and
the Cu-complex is customizable after the release of [18F]fluoride. Alterations in the [18F]fluoride
elution techniques did not have a negative effect on the subsequent
labelling reactions. We anticipate this improved [18F]fluoride elution technique to supplant the traditional azeotropic drying of [18F]fluoride in the long run and to concurrently enable the variations of the copper-complex.

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