A Conceptually New and Straightforward Method for the One-pot Transformation of Alcohols into Amines

Abstract A conceptually new amination method of alcohols has been developed using α-hydroxy esters as substrates and N-phenyl BIS-trifluoromethanesulfonimide (PhNTf 2 ) as a test reagent. Playing two roles at once, PhNTf 2 activates the hydroxyl group as a highly reactive triflate intermediate and introduces the amino functionality through an in situ nucleophilic substitution by the anionic residue PhTfN - . Two complementary procedures (methods A and B herein) have been developed, the latter permitting reaction of substrates with unstable alcoxides.