Dynamic kinetic Transfer hydrogenation reaction of 2-methyl-2, 4-diaryl-2, 3-dihydrobenzo [b][1, 4] diazepines, using phosphoric acids as catalysts and Hantzsch ester as hydride source, has been studied. A 3, 3′-H8-binol derived phosphoric acid has been identified the optimal chiral catalyst for this transformation, affording 1, 3-diamine derivatives with up to 8/1 dr, 86% ee and 94% ee for the major and minor diastereomers, respectively.
