As an important scaffold in pharmaceuticals and functional molecules, α-aminoboron compounds have received growing research interest in recent years. Despite this, the synthesis of α-aminoboron compounds still faces challenges, including the stability issues of many three-coordinate α-aminoboronates and the limited structural diversity of accessible α-aminoboranes. Herein, we report a new strategy for the synthesis of stable four-coordinate α-aminoboranes via a straightforward copper-catalyzed hydroboration of imines with neutral sp2-sp3 diboron reagents, recently developed by our group. In addition to N-aryl α-aminoboranes, this method provides one-step access to stable N-alkyl α-aminoboranes, which are challenging to synthesize using other methods.
Lou et al. (Tue,) studied this question.