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001023777 1001_ $$0P:(DE-Juel1)191040$$aBertram, Jan$$b0
001023777 245__ $$aDesmethyl SuFEx-IT: SO2F2 - Free Synthesis and Evaluation as a Fluorosulfurylating Agent
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001023777 520__ $$aAccess to SuFExable compounds was remarkably simplified by introduction of the solid FO2S-donor SuFEx-IT. However, the published process for preparation of this reagent relies on the use of sulfuryl fluoride (SO2F2), which is difficult to obtain and highly toxic. Herein, we disclose a simple protocol for SO2F2-free, hectogram-scale preparation of the analogous desmethyl SuFEx-IT from inexpensive starting materials. The reagent was prepared in a high (85%) total yield and without chromatographic purification steps. In addition, we demonstrate the utility of desmethyl SuFEx-IT by successful preparation of a series of fluorosulfates and sulfamoyl fluorides in high to excellent yields. As such, our work recognizes desmethyl SuFEx-IT as a valuable alternative to common FO2Sdonors and enables cost-efficient access to substrates for SuFEx click chemistry.
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001023777 7001_ $$0P:(DE-Juel1)175142$$aNeumaier, Felix$$b1
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001023777 7001_ $$0P:(DE-Juel1)166419$$aNeumaier, Bernd$$b3$$eCorresponding author
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