The invention relates to a method for synthesizing a flavone
alkyl phosphate compound and application thereof in a
cholesterol esterase inhibitor, which overcomes the disadvantages of the traditional method that CCl4 is used as a
solvent for synthesizing organic
phosphate, while flavone usually has a low
solubility in CCl4 and thus is difficult to carry out a
phosphorylation reaction in CCl4. In the method, DMSO (Dimethylsulfoxide), DMF (
Dimethyl Formamide),
acetonitrile,
diethyl ether, dioxane, THF (
Tetrahydrofuran), and the like, which have stronger polarity are used as solvents, and flavone has high
solubility in the solvents; nitrogenous bases, such as
triethylamine,
diethylamine,
pyridine, and the like, are used as alkali reagents; ClPO (OEt)2 (
Diethyl Chlorophosphate) is used as a
phosphorus esterification
reagent; and DMAP (Dimethylaminopyridine) is used as a catalyst. Thus, the method has the advantages of high compounding
reaction speed, mild
reaction conditions, high chemical selectivity, high reaction efficiency and higher yield of a flavone
phosphate compound with a novel structure. The new compound has the advantages of simple separation and purification method, high currency and low production cost, and the conditions required in the whole process from synthesis to separation and purification are suitable for condition requirements on production in a large scale. The new synthesized compound can be applied to preparing the
cholesterol esterase inhibitor with a
high activity, and the active IC50 of the
cholesterol esterase inhibitor is within 3.76-390nM and shows a very obvious structure-activity relationship.