Objective: To study the Synthesis process of morphine-6-β-D-glucuronic acid glycosides. Methods: Using morphine sulfate as raw material, 3-benzoyl morphine was prepared by esterification reaction. Using 1, 2, 3, 4-four-O-acetyl-β-D-glucuronic acid Me ester as raw material, the intermediate 1-three fluorine acetyl groups and 2,3,4-three-O-acetyl-β-D-glucuronic acid Me ester was prepared by ester exchange reaction. The intermediate 4 was coupled with intermediate 6, followed by glycosidic reaction to give 3-benzoyl acetyl glycoside(7), and then morphine-6-β-D-glucuronic acid glycosides was prepared by hydrolysis reaction. Results: The structure of M6 G was confirmed by ∼1H-NMR, ∼(13)C-NMR, high resolution MS and X-ray diffraction, with an overall yield of 40.3%. The purity was 99.8% determined by HPLC.Conclusion: This synthetic process has advantages of easy operation, good quality, high yield of total product, high yield and stable quality of glycosidic reaction, and is suitable for industrial production