The invention relates to polysubstituted aromatic
diketone compounds as shown in the formula (I) as well as a preparation method and application thereof. R1 in the formula (I) is a
substituent group expressed by the formula (I-1), (I-2) or (I-3), and R2 is -H, -F, -Cl, -Br, -CH3 or -OCH3. When R1 is the formula (I-1), the preparation method comprises the following steps: with 2,4-dihydroxyacetophenone as the
raw material, enabling the 2,4-dihydroxyacetophenone to be reacted with bromoacetaldehyde
ethylene acetal to obtain 1-(4-(2,2-methoxyethoxy)-2-hydroxyphenyl) ethyl
ketone; then, cyclizing and enabling the 1-(4-(2,2-methoxyethoxy)-2-hydroxyphenyl) ethyl
ketone to be reacted with
aryl chloride; finally, rearranging under an alkaline condition to obtain the polysubstituted aromatic
diketone compounds. When R1 is the formula (I-2), the method disclosed by the invention is basically same as the method adopted when R1 is the formula (I-1). When R1 is the formula (I-3), the method comprises the following steps: with
phloroglucinol as the
raw material, methylating to obtain 1,3,5-trimethoxybenzene; then, enabling the 1,3,5-trimethoxybenzene to be reacted with
acetyl chloride to obtain 1,1'-(2-hydroxy-4,6-dimethoxy-1,3-
phenylene) diethyl
ketone; next, enabling the 1,1'-(2-hydroxy-4,6-dimethoxy-1,3-
phenylene) diethyl ketone to be reacted with
aryl chloride; finally, rearranging under an alkaline condition to obtain the polysubstituted aromatic
diketone compounds. The polysubstituted aromatic diketone compounds have an inhibiting effect for HIV-1 (
Human Immunodeficiency Virus-1)
integrase. The formula (I) is shown in the specification.