The invention provides a benzopyranyl-3-alcohol esterified derivative and a preparation method of the benzopyranyl-3-alcohol esterified derivative. The benzopyranyl-3-alcohol esterified derivative is shown as the following formula I, wherein in the formula I, R represents one or more of hydrogen, hydroxy, alkoxy, alkyl amino, alkyl acylamino, fluorine or benzoyl; the benzoyl contains one or more of hydroxy, alkoxy, alkyl amino, alkyl acylamino or fluorinated substituents, wherein alkyl in alkoxy, alkyl amino and alkyl acylamino is C1 to C10 straight chain or branched chain alkyl; X in the formula represents hydrogen or oxygen; and Y in the formula represents oxygen or nitrogen and hydrogen. The benzopyranyl-3-alcohol esterified derivative is low-toxic, has excellent antineoplastic multidrug resistance activity and can be used for preparing a medicament for treating breast cancer, colon cancer, prostatic cancer, leukemia, myeloma, pancreatic cancer and the like.