abstract |
The invention discloses a synthesis method of morphine-6-beta-D-glucuronide and an intermediate compound thereof. The method comprises the steps of: (1) reacting 3-acetylmorphine and acyl-protected glucuronide in an organic solvent 1 under Lewis acid catalysis to obtain an intermediate shown in formula (IV); (2) The intermediate represented by formula (IV) is hydrolyzed with lithium hydroxide in a mixture solvent of C1-C4 alkanol and water, neutralized with hydrobromic acid, washed with C1-C4 alkanol, and dried to obtain final product; formula The definition of the substituents in (III) and (IV) is detailed in the specification. The synthesis method of the invention has the advantages of simple operation, mild conditions, high yield and easy industrialization. |