- The preparation method of the budesonide
-
The invention discloses a preparation method of budesonide. The preparation method comprises the following steps: (1) carrying out n-butyraldehyde aldolization for 16 alpha-hydroxyl prednisolone acetate as shown in formula (1) to obtain a budesonide crude prodct; (2) then hydrolyzing 21-acetates; and (3) collecting the product budesonide from reactant. By adopting the preparation method, the unstable midbody 16 alpha-hydroxyl prednisolone is avoided. The preparation method is easy to operate and control, and the total yield of the budesonide is greatly increased. The reaction formula is shown in the specification.
- -
-
Paragraph 0039; 0040; 0041; 0044
(2017/11/16)
-
- A preparation method of budesonide
-
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.
- -
-
Paragraph 0061; 0062; 0063; 0072
(2017/08/25)
-
- A kind of budesonide S isomer R isomer method of preparation
-
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.
- -
-
Paragraph 0008; 0018
(2017/01/12)
-
- PHOSPHATE BASED LINKERS FOR INTRACELLULAR DELIVERY OF DRUG CONJUGATES
-
Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).
- -
-
Page/Page column 73
(2015/11/18)
-