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18F-Trifluoromethylation of Unmodified Peptides with 5-18F-(Trifluoromethyl)dibenzothiophenium Trifluoromethanesulfonate.

Stefan VerhoogChoon Wee KeeYanlan WangTanatorn KhotavivattanaThomas C WilsonVeerle KersemansSean SmartMatthew TredwellBenjamin G DavisVéronique Gouverneur
Published in: Journal of the American Chemical Society (2018)
The 18F-labeling of 5-(trifluoromethyl)-dibenzothiophenium trifluoromethanesulfonate, commonly referred to as the Umemoto reagent, has been accomplished applying a halogen exchange 18F-fluorination with 18F-fluoride, followed by oxidative cyclization with Oxone and trifluoromethanesulfonic anhydride. This new 18F-reagent allows for the direct chemoselective 18F-labeling of unmodified peptides at the thiol cysteine residue.
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