The asymmetric synthesis of S-and R-bisoprolol fumarate, a selective β₁-blocker inhibitor with extensive clinical use, is presented in this paper. Firstly R-and S-epichlorohydrin is used as chiral reagent to directly react with 4-((2-isoproxyethoxy)methyl)-phenol, then further react with isopropylamine, finally react with fumarate to give the target product S-and R-bisoprolol fumarate with a total yield of 60.8% and an ee value is higher than 92%.