The invention relates to the field of
organic synthesis, in particular to a synthesis method of gamma-aminophosphine
oxide compounds and derivatives thereof. According to the synthesis method disclosed by the invention, alpha, beta-unsaturated
amide, diaryl
phosphine oxide or
phosphite ester is taken as raw materials, and under the action of acid, the gamma-aminophosphine
oxide compound can be rapidly and efficiently synthesized by a one-pot method. The preparation method comprises the following steps of: generating conjugated
nitrile positive ions or
imine salt intermediates with strong electrophilicity from alpha, beta-unsaturated
amide under the activation of acid, converting diaryl
phosphine oxide or
phosphite ester into strong nucleophilic three-coordination
phosphorus species under the action of alkali, and further performing
phosphorus-doped Michael
addition reaction on the conjugated intermediates to finally generate the gamma-aminophosphine oxide compounds. According to the method disclosed by the invention, diaryl
phosphine oxide or phosphite which is cheap, easy to obtain and stable in
structural property is used as a
phosphorus source, the substrate applicability is wide, and the economic cost is relatively low; in addition, the method realizes synthesis of a target product without participation of a
metal catalyst, and is rapid and efficient.