The invention relates to synthesis of a series of tacrine-caffeic acid hetero-blends and derivatives, a preparation method thereof, medicinal compositions containing them, and their medical application. The structural formula of the tacrine-caffeic acid hetero-blends is shown as formula (I). By changing substituent groups and joints, the inhibitory activity to AChE (acetylcholinesterase) and selectivity to AChE/BuChE (butyrocholinesterase), as well as antioxidant activity can be adjusted. And AChE-induced Abeta (amyloid-beta peptide) aggregation can be inhibited. The tacrine-caffeic acid hetero-blends and derivatives can be prepared into appropriate medicinal dosage forms to treat Alzheimer's disease and other related dementia. The invention belongs to the medical field.

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