Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides.
Wright M., Martínez-Lamenca C., Leenaerts JE., Brennan PE., Trabanco AA., Oehlrich D.
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.