1106-03-2Relevant academic research and scientific papers
Preparation method of methyl metacortandracin
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Paragraph 0010; 0012-0014, (2017/11/18)
The invention discloses a preparation method of methyl metacortandracin. The methyl metacortandracin is prepared by taking 16-b methyl-9 (11) a-epoxy-prednisolone acetate (called as DB11 for short) as a raw material; dissolving the raw material in an organic solvent and reacting with hydrobromic acid to obtain bromine hydroxyl content 9a bromine-16b methyl-prednisolone acetate; performing catalytic hydrogenation and 9-bit debromination on bromine hydroxyl content in the organic solvent by acid-binding agent and palladium carbon to obtain a debromination matter 16b methyl-metacortandracin; oxidizing the debromination matter with strong oxidant in the organic solvent to obtain prednisolone acetate; finally, hydrolyzing the prednisolone acetate in the organic solvent by catalyst to obtain methyl metacortandracin. The total weight yield through four-step synthesis is 52-55%. The production method is wide in raw material source, economic and environment-friendly in technique, short in synthesis route, and high in production yield; the production cost is 30-40% lower than that of the traditional method, and 15-20% lower than the method of application number 201610952306.6; the technique is simple and convenient; the solvent can be recycled and used indiscriminately; the preparation method is easy to practice the industrial production.
