Copper(I) Catalyzed Regioselective Asymmetric Alkoxyamination of Aryl Enamide Derivatives

The copper(I) catalyzed reaction of an enamide with an iminoiodane, in the presence of an alcohol, triggers the direct alkoxyamination of the double bond. This transformation represents a straightforward access to α-amino aminals in a completely regio- and diastereoselective manner. Use of a chiral Box ligand allows this reaction to be carried out in an enantioselective fashion.

在醇类存在的条件下，经一价铜（copper(I)）催化的烯酰胺（enamide）与亚胺碘烷（iminoiodane）发生反应，可引发双键的直接烷氧基胺化（alkoxyamination）。该转化能够以完全的区域选择性与非对映选择性路径，便捷地合成α-氨基缩醛胺（α-amino aminal）。若使用手性双恶唑啉（Box）配体，则可实现该反应的对映选择性合成。