The invention relates to a synthesis method of 5, 7, 4'-trihydroxy-3', 5'-dimethoxyflavone and application thereof, particularly to a chemical synthesis method of allelochemicals, 5, 7, 4'-trihydroxy-3', 5'-dimethoxyflavone, by separating from allelochemical rice, Oryza sativa L.(PI312777). Syringic acid and phloroglucinol are used as the raw materials, the object products are synthesized by four steps. The products are protected by benzyl, and benzyl is synchronously removed with glacial acetic acid heating and ring closing in the final reaction step, thereby reducing the reaction steps. Compared with the method of removing benzyl by Pd / C charging hydrogen, the method of the invention is more simple, economical, and safe. The invention is capable of effectively stopping growth of garnyardgrass, cyperus iria linn and cyperus difformis linn seeds in rice, restraining paddyfield weed, improving rice yield, stopping spore germination of pyricularia oryzae and rhizoctonia solan so as to avoid the problems due to pesticide application and promote sustainable development of agriculture.