The invention relates to a preparation method of a nerve regeneration amide medicine. The method is characterized in that the nerve regeneration amide medicine is prepared from o-methoxyaniline and ethyl glyoxalate through a four-step reaction, and the method concretely comprises the following steps: carrying out a reductive amination reaction on the raw materials comprising o-methoxyaniline and ethyl glyoxalate to obtain an intermediate I, reacting the intermediate with p-toluensulfonyl chloride to obtain an intermediate II, hydrolyzing the intermediate II to obtain an intermediate III, and reacting the intermediate III with 3-amino-4-methoxypyridine to obtain the final product. The preparation method has the advantages of low irritation in the synthesis reaction process, convenience in production and high molecule yield, and is a 2-[(2-methoxyphenyl)-(4-methylbenzenesulfonyl)]amino-N-(4-methoxypyridyl)-3-acetamide production method suitable for industrial production.