The invention discloses a synthetic method for 2-substituted-1,4-naphthoquinone derivatives. The method comprises the following steps: with 2-alkynylacetophenone compounds as shown in a formula I which is described in the specification as a raw material and dimethyl sulfoxide as an oxidizing agent and a solvent, carrying out a reaction at 80 to 140 DEG C under stirring and the action of a copper catalyst for 2 to 10 h; and subjecting a reaction solution obtained after completion of the reaction to post-treatment so as to obtain the 2-substituted-1,4-naphthoquinone derivatives as shown in a formula II which is described in the specification, wherein the copper catalyst is a mixture of bis(copper trifluoromethanesulfonate) and an inorganic cuprous salt, and the inorganic cuprous salt is one selected from a group consisting of cuprous iodide, cuprous chloride, cuprous bromide and cuprous cyanide. The method has the advantages that the raw materials are variable; the number of the prepared derivatives is great; the catalyst is cheap and easily available; cost is substantially reduced; no pollution is produced; no extra oxidizing agent is needed; dimethyl sulfoxide both functions as the oxygen source and the solvent, so cost is saved; and the method has the characteristics of high reaction yield, good substrate applicability, simple operation, etc.