The invention discloses a synthesis method of a polysubstituted 1,3-dihydronaphtho[2,3-c]furan derivative. The synthesis method comprises the following steps: in the presence of a metal salt and an organic solvent, carrying out an intermolecular self-coupling cyclization reaction on a 3-aryl-2-propyn-1-ol compound, and after the reaction is finished, carrying out post-treatment to obtain the polysubstituted 1,3-dihydronaphtho[2,3-c]furan derivative. According to the invention, reaction conditions are mild and simple, only a catalytic amount of the metal salt needs to be added, and other additives and ligands do not need to be added; the reaction process does not need anhydrous and anaerobic conditions, operation is simple and convenient, reaction time is short, reaction yield is high, andthe adaptability of a reaction substrate is good; and meanwhile, only water is produced as a by-product in the preparation method, so the preparation method has higher atom economy. In addition, an amplification experiment of the preparation method disclosed by the invention can be well realized, so the preparation method can meet requirements for large-scale application and development in the fields of biological medicines and the like.