51333-05-2Relevant articles and documents
A preparation method of budesonide
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Paragraph 0061; 0062; 0063; 0072, (2017/08/25)
The invention discloses a budesonide preparing method. Prednisone I and acetic anhydride II react to produce 17,21-diacetoxy-1,4-pregnane diene-3,11,20-triketone III, the III is degreased in an anhydrous solvent to obtain 21-acetoxyl group-1,4,16-pregnane diene-3,11,20-triketone IV, the IV is oxidized to obtain 16alpha,17alpha-dyhydroxy-21-acetoxyl-1,4-pregnane diene-3,11,20-triketone V, the V and n-butyl aldehyde VI are condensed to obtain 16alpha,17alpha-22(R,S) propyl methylenedioxy-21-acetoxyl group-1,4-pregnane diene-3,11,20-triketone VII, the VII is reduced to obtain 16alpha,17alpha-22(R,S) propyl methylenedioxy-11beta-hydroxyl-21-acetoxyl group-1,4-pregnane diene-3,20-diketone VIII, the VIII is subjected to base catalysis to obtain budesonide IX. The budesonide preparing method is suitable for industrial production.
A kind of budesonide S isomer R isomer method of preparation
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Paragraph 0008; 0018, (2017/01/12)
The invention discloses a method for preparing an R-isomer by using an S-isomer of budesonide. The method comprises the steps: enabling budesonide and acetic anhydride to be subjected to esterification reaction to obtain budesonide acetate; then, carrying out oxidative ring cleavage under the action of a strong oxidant to obtain 16-alpha hydroxyprednisonlone acetate; and condensing butyraldehyde and the 16-alpha hydroxyprednisonlone acetate to obtain budesonide acetate, and hydrolyzing to obtain R-budesonide. The method disclosed by the invention is high in conversion rate, high in yield and capable of effectively converting the S-isomer of the budesonide into the R-isomer.