Abstract

AbstractA copper‐phosphine system (Cu(OAc)2 and t‐Bu3P⋅HBF4) was used to synthesize α‐aminophosphonates and phosphoramides from various aromatic amines and trialkyl phosphites under oxygen atmosphere. With this Cu−P system, α‐aminophosphonates containing C−P bonds were generated from N,N‐dimethylanilines or N‐methylanilines and trialkyl phosphites; phosphoramidates containing N−P bonds were produced from N‐benzylanilines and trialkyl phosphites. This strategy provided a convenient and efficient method for the synthesis of phosphorous compounds. The compounds containing phosphoryl group attracted extensive attention due to their biological activities and wide applications.[1,2] The α‐aminophosphonates have been applied in medicine and agriculture such as anticancer drugs, antibiotics, antibacterial agents, and enzyme inhibitors.[1] And phosphoramides could be served as antibiotics, prodrugs, flame retardants, and ligands.[2]

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