The invention discloses a croton acylated catapol derivative which is prepared by esterifying catalpol and crotonic anhydride. The invention provides a corresponding preparation method and application, and the preparation method comprises the following steps: 1) dissolving catalpol into triethylamine, adding a catalyst 4-dimethylaminopyridine, adding crotonic anhydride under protection of nitrogengas, reacting for 12-36 hours at a temperature of 30-90 DEG C, and drying triethylamine by distilling to obtain a product, wherein a molar ratio of crotonic anhydride to catalpol is (6-18) to 1, anda molar ratio of 4-dimethylaminopyridine to catalpol is 1 to (9.5-10.5); and 2) dissolving the product in the step 1) into dichloromethane, adding an alkaline agent, standing and layering, discardingan upper-layer water phase, drying an organic phase to remove water, drying dichloromethane by distilling, purifying and separating, evaporating-drying, and filtering to obtain the catapol derivative.The catapol derivative has good anti-ageing activity, improves blood-brain barrier permeability of catapol, and has an esterification rate of 99.16%.