Abstract: A synthesis route to produce ethyl (R)-2-hydroxy-4-phenylbutyrate, an important intermediate for several ACE inhibitors is described starting from acetophenone and diethyl oxalate. Ethyl 2,4-dioxo-phenylbutyrate is synthesized from acetophenone and diethyl oxalate by using different conditions,the optimal condition is founded. The reaction was run in aqueous toluene at 30℃ for 2h under the catalysis of Sodium ethoxide. The yield is 39.1%. Also the condition of the hydrogenation of ethyl 2,4-dioxo-4-phenylbutyrate catalyzed by a heterogeneous Raney Ni catalyst is studied . The effects of modifier amount, reaction time, hydrogen pressure and temperature on enantiometric excess are investigated to synthesize ethyl (R)-2-hydroxy-4-
phenylbutyrate. It is found that conversation and enantioselectivity showed a maximum in the condition of modifier amount is 7mg for 150min. The conversation increased with the increase of reaction time,which almost had no effect on the enantioselectivity, but it had adverse influence on enantiomeric excess. The study provides a practicable method for industrial production of this remedy.