Abstract: A preparation method for a morpholine-based organophosphine ligand includes the steps of: adding 1,3-dibromobenzene, morpholine, an inorganic base, and a first catalyst to a reactor under a nitrogen (N2) atmosphere, and using tetrahydrofuran (THF) as a reaction solvent; reacting a mixture at 45-55° C. for 5-7 h; lowering a reaction temperature to ?75 to ?80° C., and adding n-butyllithium (nBuLi); and raising the reaction temperature to 0° C. after stirring, and adding a second catalyst and a halophosphine reagent for reaction to obtain a morpholine-based organophosphine ligand. A method for synthesizing novel morpholine-based organophosphine ligands under mild conditions of the present disclosure has been successfully applied in palladium (Pd)-catalyzed carbon-nitrogen (C—N) bond formation reactions, demonstrating high efficiency and selectivity, simplifying reaction conditions, and broadening the scope of application.