A novel synthetic approach towards 5-fluoro-2-hydroxy butyrophenone is reported. Using 4-fluorophenol as a raw material, the processes of etherification protection, Friedel-Crafts acylation and demethylation provide the target compound under mild conditions. The structure was characterized by the melting point and IR, MS,1H-NMR, and13C-NMR spectroscopy. The bioassay results indicate that the target compound exhibits potent antifungal activities againstValsa mali,Coniella dipodiella, and other agricultural plant fungi. The target compound also shows potent herbicidal activities forLactuca sativa, a dicotyledon, andEchinochloa crus-galli, a monocotyledon. The toxicity regression C50values of the compound againstValsa mali,Coniothyrium diplodiella,Lactuca sativaseedling, andEchinochloa crusgalliseedling were calculated by SPSS. The Hormesis effect for roots ofEchinochloa crusgalliwas confirmed.