The synthesis of 3-(N-ethyl-N-methoxycarbonylmethyl)amino acetanilide was reported by 3-aminoacetanilide as starting material via two step reactions. The desired product was yield by the ethylated compound (from 3-aminoacetanilide reacted with acetaldehyde) reacted with methyl chloroacetate. The optimized reaction conditions were as follows: In the first step, The yield of 3-(N-ethyl)amino acetanilide was 90.7% and its purity was up to 97.5%, when the molar rate of acetaldehyde to 3-aminoacetanilide was 1.2 and 5% Pd/C as catalyst under 3.5MPa of hydrogen atmosphere at 70℃. In the second step, the desired product was obtained in 94.6% yield and 96.8% purity with 0.6 equiv. of sodium carbonate as deacid reagent under 70 ℃.