N-Thiophosphoryl imines: convenient substrates in the aza-Henry reaction

In the presence of 1,1,3,3-tetramethylguanidine (TMG), N-diethoxythiophosphorylimines 1 and N-diphenylthiophosphinoylimines 2 exhibited good reactivity in the aza-Henry reaction. The corresponding products were obtained in excellent chemical yields under mild conditions. Moreover, the asymmetric version of the N-thiophosphoryl imine 1-based aza-Henry reaction was also realized with ee values up to 87% by employing Takemoto’s thiourea as the catalyst.