Thermal Effects in the Organocatalytic Asymmetric α-Amination of Disubstituted Aldehydes with Azodicarboxylates: A High-Temperature Organocatalysis

This article describes the thermally accelerated organocatalytic α‐amination of disubstituted aldehydes with azodicarboxylates under microwave conditions. Compared to the results previously obtained at room temperature, both yield and enantioselectivity could be significantly increased. Employing microwave irradiation resulted in a considerably reduced reaction time. Therefore, this improved protocol allows the fast and efficient synthesis of α,α‐disubstituted amino aldehydes and provided the best results for the α‐amination of disubstituted aldehydes to date. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008) A case of thermally accelerated organocatalytic α‐amination of disubstituted aldehydes is presented. Compared to the results previously obtained at room temperature, both yield and enantioselectivity could be significantly increased. This improved protocol allows the fast and efficient synthesis of α,α‐disubstituted amino aldehydes.