The invention discloses a compound with anti-alzheimer's disease activity which has a structure in formula (I), and the substituent R of the compound represents C1-C6 alkyl group, cycloalkyl group or aryl group. By structurally transforming the C-5 site of L-685-458, the method is adopted for the first time to successfully prepare the L-685-458, synthesize five types of new L-685-458 analogues, which have the advantages of high yield, easiness in separation, low cost, convenient production expansion and the like. Inferred according to the activity of the compound L-685-458, the five types of new L-685-458 analogues ought to have the anti-alzheimer's disease activity, and therefore have the prospect of being developed into anti-alzheimer's disease medicines.