Abstract: The intermediate 1-isopropyl-5-methoxy-benzimidazolone（4） was prepared starting from 4-methoxy-2-nitroaniline（1） via alkylation,reduction of nitro group and cyclization reactions,and twenty-four benzimidazolone derivatives(5a~5x) were finally obtained by N-acylation with a variety of acyl groups.The structures of the new synthesized derivatives were confirmed by 1H NMR and elemental analysis.Antifungal activity tests indicated that all of the title compounds exhibited variable inhibitory activitiy against the spore germination of Botrytis cinerea,and the inhibition rates of the most potential compounds 5i and 5q at the concentration of 50 μg/mL were 95.9% and 93.4%,respectively.