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000907585 1001_ $$0P:(DE-Juel1)180982$$aWalter, Nils$$b0
000907585 245__ $$aConvenient PET-tracer production via SuFEx 18F-fluorination of nanomolar precursor amounts
000907585 260__ $$aAmsterdam [u.a.]$$bElsevier$$c2022
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000907585 520__ $$aRecently, a protocol for radiolabeling of aryl fluorosulfates (“SuFEx click radiolabeling”) using ultrafast18F/19F isotopic exchange has been reported. Although promising, the original procedure turned out to berather inefficient. However, systematic optimization of the reaction parameters allowed for developmentof a robust method for SuFEx radiolabeling which obviates the need for azeotropic drying, base additionand HPLC purification. The developed protocol enabled efficient 18F-fluorination of low nanomolaramounts of aryl fluorosulfates in highly diluted solution (micromolar concentrations). It was successfullyused to prepare a series of 29 18F-fluorosulfurylated phenols e including modified ezetimibe, atocopheroland etoposide, the two tyrosine derivatives Boc-Tyr([18F]FS)-OMe and H-Tyr([18F]FS)-OMe,the FAP-specific ligand [18F]FS-UAMC1110, and the DPA-714 analog [18F]FS-DPA e in fair to excellentyields. Preliminary evaluation demonstrated sufficient in vivo stability of radiofluorinated electron rich orneutral {Boc-Tyr([18F]FS)-OMe), H-Tyr([18F]FS)-OMe and [18F]FS-DPA} aryl fluorosulfates. Furthermore,[18F]FS-DPA was identified as a promising tracer for visualization of TSPO expression
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000907585 7001_ $$0P:(DE-Juel1)191040$$aBertram, Jan$$b1
000907585 7001_ $$0P:(DE-Juel1)131817$$aDrewes, Birte$$b2
000907585 7001_ $$0P:(DE-Juel1)172894$$aBahutski, Victor$$b3
000907585 7001_ $$0P:(DE-HGF)0$$aTimmer, Marco$$b4
000907585 7001_ $$00000-0003-3381-2729$$aSchütz, Markus B.$$b5
000907585 7001_ $$0P:(DE-Juel1)186984$$aKrämer, Felicia$$b6
000907585 7001_ $$0P:(DE-Juel1)175142$$aNeumaier, Felix$$b7$$eCorresponding author
000907585 7001_ $$0P:(DE-Juel1)180330$$aEndepols, Heike$$b8
000907585 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b9$$eCorresponding author
000907585 7001_ $$0P:(DE-Juel1)176188$$aZlatopolskiy, Boris D.$$b10
000907585 77318 $$2Crossref$$3journal-article$$a10.1016/j.ejmech.2022.114383$$bElsevier BV$$d2022-07-01$$p114383$$tEuropean Journal of Medicinal Chemistry$$v237$$x0223-5234$$y2022
000907585 773__ $$0PERI:(DE-600)2005170-0$$a10.1016/j.ejmech.2022.114383$$gVol. 237, p. 114383 -$$p114383$$tEuropean journal of medicinal chemistry$$v237$$x0223-5234$$y2022
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