The synthesis of α-aryl-α-aminophosphonates was performed by the three-component Kabachnik-Fields reaction of primary amines, benzaldehyde derivatives and dialkyl phosphites in a continuous flow microwave reactor. The target compounds could be obtained in high (~90%) yields without any catalyst in simple alcohols as the solvent. The flow process elaborated required shorter reaction times and lower excess of the reagent, as compared to the “traditional” batch reactions, and allowed the synthesis of the α-aminophosphonates on a somewhat larger scale.
The synthesis of dialkyl H-phosphonates and α-aminophosphonates was studied in a continuous flow microwave reactor. Depending on the conditions, the alcoholysis of dialkyl H-phosphonates could be fine-tuned towards the mixed and the fully transesterified products. The continuous flow synthesis of α-aryl-α-aminophosphonates was elaborated utilizing the aza-Pudovik reaction of imines and dialkyl H-phosphonates, as well as the by the Kabachnik-Fields condensation of primary amines, benzaldehyde and >P(O)H reagents.
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