Copper-Catalyzed a-Animation of Phosphonates and Phosphine Oxides: A Direct Approach to a-Amino Phosphonic Acids and Derivatives

摘要

A direct approach to important a-aminophosphonic acids and its derivatives has been developed by using copper-catalyzed electrophilic amination of a-phosphonate zincates with O-acyl hydroxylamines. This amination provides the first example of C~N bond formation which directly introduces acyclic and cyclic amines to the a-position of phosphonates in one step. The reaction is readily promoted at room temperature with as little as 0.5 mol % of catalyst, and demonstrates high efficiency on a broad substrate scope.