C2-symmetric BINOL-squaramide as efficient organocatalyst for the enantioselective α-amination of 1,3-dicarbonyl compounds with dialkyl azodicarboxylates

The asymmetric α-amination of 1,3-dicarbonyl compounds with dialkyl azodicarboxylates has been achieved by C2-symmetric BINOL-squaramide bearing multiple hydrogen bond donors to provide the desired products in excellent yields and enantioselectivities (up to 99% yield and 98% ee).

Graphical abstractThe asymmetric α-amination of 1,3-dicarbonyl compounds with dialkyl azodicarboxylates has been achieved by C2-symmetric BINOL-squaramide bearing multiple hydrogen bond donors to provide the desired products in excellent yields and enantioselectivities (up to 99% yield and 98% ee).Figure optionsDownload full-size imageDownload as PowerPoint slide