The invention belongs to the fields of a chemical substance and medicine preparation, and relates to multi-target treatment mild cognitive impairment medicine (R)-ladostigil R-type chiral intermediate and an analogue preparation and an application thereof. A substrate compound 3 and an acyl donor 7 are reacted under alkaline condition, a palladium catalyst and enzyme are reacted through dynamic kinetic resolution (DKR) under catalysis to obtain a compound 4 (the ladostigil R-type chiral intermediate and its analogue), and the prepared ladostigil R-type chiral intermediate and its analogue are used for preparing ladostigil. The synthetic method has the advantages of advantages of short route, low cost, mild condition, good stereoselectivity, high yield and little environmental pollution, and accords with green chemistry requirement.