- Methylprednisilone preparation method (by machine translation)
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Methylprednisilone preparation method, is made up of 4 - androstenedione (abbreviated as 4AD) preparation of the 16 (17) a - epoxy prednison in organic solvent with the glycol in 10 - 50 °C shall ketal acid catalyzed reaction: 20 - shrinks the keto - 16a (17) - epoxy prednison; then the ketal in organic solvent with the three a chlorosilane silicon ether alkali catalytic reaction shall be: 21 - a silicon ether base - 20 - shrinks the keto - 16a (17) - epoxy prednison; then the silicon ether in organic solvent with the 2M methyl magnesium halide Grignard reaction, in the strong acid in the resulting standard hydrolyze methylprednisilone, HPLC content detected 99.0% or more, melting point 228 - 237 °C, synthetic weight total yield of 80 - 85%. To the invention producing methyl prednisone, raw material sources are extensive, process economic and environmental protection, simple and convenient production operation, short synthetic route, synthetic high yield, low production cost compared to the conventional method of 30 - 40%; is favorable for industrial production. (by machine translation)
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Paragraph 0013
(2017/04/28)
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- Preparation method of methyl metacortandracin
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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.
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- Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
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Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.
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