The invention relates to the technical field of biological medicines, and particularly discloses a synthesis method of cibopadol citrate, which has the advantages that no toxic
solvent is used in the synthesis process, the environmental
pollution is reduced, and the cost is reduced; the purification process of the intermediate in the synthesis process is simplified, so that the operation process is simplified, and the actual production is easier; a common
solvent is used in the
crystallization salt forming process, the operation process is simple, and industrial production is facilitated; the citrate can promote the
medicine to be better released
in vivo by improving the
solubility of the
medicine, so that the utilization degree and the effect of the
medicine are improved; the citrate has better
chemical stability, so that the citrate has better preparation stability; in addition, by optimizing the release characteristics of the
drug (e.g., improving the sustained release mechanism), the citrate form may play a positive role in reducing the side effects of the
drug.