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Bench-stable transfer reagent facilitates the generation of trifluoromethyl-sulfonimidamides

By M Wright, C Martínez-Lamenca, JE Leenaerts, PE Brennan, AA Trabanco and D Oehlrich


Sulfonimidamides are an emerging bioisosteric replacement in medicinal chemistry projects, and therefore new chemistries are necessary to access this functionality. The general synthesis of CF3-sulfonimidamides from an activated bench-stable transfer reagent is described. A diverse reaction scope is demonstrated, with a wide range of nucleophilic amines being tolerated in this transformation. The CF3-sulfonimidamides obtained contain an additional diversity point, in the form a protected imine, that could be unmasked to allow late stage modifications

Topics: Journal Article
Publisher: 'American Chemical Society (ACS)'
Year: 2018
DOI identifier: 10.1021/acs.joc.8b01244
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