Abstract

A direct approach to access important α-amino phosphonic acids and their derivatives through the formation of C–N bonds is described. Several α-amination reactions of phosphonates that involve electrophilic aminating agents are reviewed. A recent development is highlighted in which an acyclic or cyclic amine is introduced into the α-position of a phosphonate in one step through deprotonative formation of an α-zincate followed by copper-catalyzed amination with an <i>O</i>-acylhydroxylamine.

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