Copper-Catalyzed Enantioselective Propargylic Amination of Nonaromatic Propargylic Esters with Amines

The enantioselective propargylic amination of propargylic pentafluorobenzoates bearing an alkyl group at the propargylic position with amines in the presence of catalytic amounts of a copper complex and an optically active diphosphine such as BINAP has been found to give the corresponding propargylic amines in good yields with high enantioselectivity.

研究发现，在催化量的铜络合物和光学活性的双磷叶立德，如BINAP的存在下，对带有位于丙炔基位置的烷基基团的丙炔基五氟苯甲酸进行对映选择性丙炔基胺化反应，能够以良好的产率和极高的对映选择性得到相应的丙炔基胺。