To improve the solubility of ergosterol, the ergosteryl lipoate was prepared by a chemical method under ambient temperature, and the antioxidation of ergosteryl lipoate in oil was studied. By single factor experiments, the optimum conditions for the synthesis of ergosteryl lipoate were obtained. The conversion could be achieved 91% in the following conditions: DMAP/EDC/Et₃N as the catalyst, 80 mmol/L ergosterol, molar ratio of lipoic acid/ergosterol/DMAP/EDC/Et₃N 2.0∶1.0∶0.2∶1.2∶1.5, dichloromethane as the solvent, reaction temperature of 25 ℃, reaction time of 20 h. The solubility of ergosteryl lipoate in oil is about twice of ergosterol, and the antioxidant ability is about 1.5 times of ergosterol.