- Preparation method of triamcinolone acetonide
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The preparation method comprises the following steps: an oxidation reaction, a hydrolysis reaction, an epoxy reaction and a fluorine-containing reaction. After formic acid is added to the organic solvent acetone, a certain amount of the oxidant potassium permanganate is added after formic acid is added, and after the thin layer is analyzed to no raw material, a certain amount of the reducing liquid is added into the reactor, and after the reaction is complete, a certain amount of water is added, and after the reaction is complete 55 - 65min, the oxide is obtained by suction filtration. The method is mild in reaction condition, easy to control and small in auxiliary material toxicity. The preparation method adopts the transformation of 9, 11-position, 16,17-position and 21-position, can obtain triamcinolone, adopts the company existing products as starting materials, is short in route, easily available in raw materials, free of auxiliary materials with strong toxicity, high in yield and low in cost.
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Paragraph 0023; 0025-0027; 0031-0033; 0037-0039
(2021/10/11)
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- Preparation method of triamcinolone acetonide
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The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of triamcinolone acetonide. To the method, the epoxy compound I is taken as a raw material, 70% pyridine hydrofluoric acid solution is used as a fluorinated reagent, then the amount of hydrofluoric acid is reduced, reaction conditions are reduced, and reaction steps are optimized.
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Paragraph 0039-0044
(2021/11/21)
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- Method for preparing 16 alpha-hydroxyprednisolone
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The invention discloses a method for preparing 16 alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. According to the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione 21-acetate is used as an initial raw material and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis to prepare 16 alpha-hydroxyprednisolone. Accordingto the method for preparing 16 alpha-hydroxyprednisolone, generation of impurities in the reaction process can be effectively controlled by improving the defects of a traditional process, reaction process is mild, and an overall conversion rate is high; and the method disclosed by the invention has the advantages of low requirements on a reaction device, low operation cost, simplicity and convenience in operation, suitability for industrial production and higher market prospects.
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Paragraph 0011; 0030-0031; 0035-0036; 0040-0041
(2020/07/02)
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- A budesonide industrial preparation method (by machine translation)
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The invention relates to a cloth budesonide industrial preparation method. Specifically, the invention relates to a hydrochloric acid aqueous solution, dichloromethane and in acetonitrile, 16 α - hydroxy prednisolone with butyraldehyde by the reaction of the budesonide. In the method of the present invention has the industrial can be implemented on, repeatability and the like. (by machine translation)
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Paragraph 0039-0041
(2019/03/10)
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- Preparation process of triamcinolone acetonide
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The invention relates to a preparation process of triamcinolone acetonide. The triamcinolone acetonide is prepared by taking an intermediate III as a raw material. The preparation process comprises the following steps of: by taking a hydrofluoric acid-acetone mixed solvent as a solvent, slowly adding the intermediate III in a temperature range of 40 DEG C below zero to 30 DEG C below zero; after adding the raw material, performing a reaction for 4-8 hours; returning the temperature to 5 DEG C below zero to zero DEG C, and continuously performing a reaction for 10-30 min; after reaction, slowly adding the reaction liquid into a potassium carbonate solution; adjusting the PH value to 7.0-7.5; filtering and discharging the material; and drying the same to obtain triamcinolone acetonide. The preparation process shortens the production period, prevents use of a lot of high-matching acetone and is more environmentally friendly.
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Paragraph 0008
(2017/07/21)
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- NOVEL PROCESS FOR PREPARATION OF GLUCOCORTICOID STEROIDS
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The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula (I) wherein each substituent is independently selected from; R1 is H or CH3; R2 is C1-C6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R1 and R2 combine to form saturated, unsaturated C3-C6 cyclic or heterocyclic ring; R3 and R4 are same or different and each independently represents H or halogen; R5 is -OH or –OCOR wherein R represents H or C1-C6 linear, branched or cyclic alkyl group that may be substituted.
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Page/Page column 12; 13
(2016/08/23)
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