53 results about "Cortisone acetate" patented technology

The invention relates to a preparation method of an important intermediate of cortisone acetate, and in particular relates to a preparation method of cortisone acetate intermediate 17alpha-hydroxypregnen-4-alkene-3,11,20-triketone. The preparation method comprises the following steps of (1) preparing an oxidization reagent A; (2) oxidizing 11alpha, 17 alpha-dihydroxypregnen-4-alkene-3,20-diketone to generate 17alpha-hydroxypregnen-4-alkene-3,11,20-triketone. According to the invention, the problem that industrialized production of 17alpha-hydroxypregnen-4-alkene-3,11,20-triketone in a proper workshop is carried out is solved, so the preparation method disclosed by the invention has the characteristics of lower cost and proper yield, and is more suitable for industrialized large-scale production; the reference quality yield of the 17alpha-hydroxypregnen-4-alkene-3,11,20-triketone obtained by the preparation method is 90-100%, and the reference high performance liquid chromatography purity of the 17alpha-hydroxypregnen-4-alkene-3,11,20-triketone is 95-99.9%.

The invention relates to a method for directly generating prednisolone through bio-fermentation in one step by using cortisone acetate as a raw material and Arthrobacter Simple ATCC 21032.

The invention discloses a method for preparing prednisone acetate. The method comprises the steps that firstly, positions 1,2 of cortisone acetate is dehydrogenated by using arthrobacter simplex CPCC140451 and are converted to generate the prednisone acetate, and then mixed solvents are used for refining. The method for preparing the prednisone acetate has the advantages of simple process, high refining efficiency, simple and easy obtained solvent, recycling and low toxicity, and can be used in large-scale industrial production.

The invention relates to a preparation method of cortisone acetate. Anecortave acetate is used as a raw material and sequentially takes addition, oxidization and reduction reaction to obtain the anecortave acetate. The method comprises the following reaction steps of A, addition reaction: under the nitrogen production, adding the anecortave acetate into an organic solvent; adding a halogenating reagent and an acid catalyst to obtain an intermediate II; B, oxidization reaction: under the nitrogen gas protection, adding the compound II into the organic solvent; adding an oxidizing agent to obtain an intermediate III; C, reduction reaction: under the nitrogen gas production, adding the compound III into the organic solvent; adding an acid catalyst and a reducing agent to obtain a target product of the cortisone acetate IV. The method has the advantages that the raw materials can be easily obtained; the reaction steps are few; the quality and the yield achieve the obvious competitiveness; in addition, the pollution on the environment is reduced.

The invention discloses a preparation method of cortisone acetate. According to the method, hydrocortisone is taken as an initiator, and preparation is performed through steps including acetylation, oxidization and the like. Sodium hypochlorite which is low in cost and environment-friendly is used for replacing chromic anhydride which is high in cost and larger in toxicity and serves as an oxidizing agent in an oxidation reaction, and a catalyst which cannot be recovered and recycled is not required in an oxidation reaction process. The preparation method of the cortisone acetate has the advantages that the production cost is reduced, the production operation is simplified, environmentally hazardous chromium ion wastewater is not discharged, and the method is suitable for industrial production.

The invention discloses a preparation method of cortisone acetate, and belongs to the field of pharmaceutical chemistry. According to the method, 11 alpha-hydroxy- 16 alpha, 17 alpha-epoxy progesterone is used as a raw material to prepare the cortisone acetate through bromine reaction, debromination reaction, bromination reaction, replacement reaction and oxidation reaction. The method can effectively avoid the occurrence of side reactions, and improves the quality of the product; at the same time, iodine is replaced by low-cost bromine for halogenating reaction, the production cost is greatly reduced, the method is high in efficiency and low in energy consumption, and the product quality and yield are good.

The invention discloses a process for preparing hydrocortisone, and belongs to the field of chemical pharmacy. The process comprises the following steps of: preparing a reducing matter by using cortisone acetate as a raw material; removing a protecting group to acquire the hydrocortisone; in the step of removing the protecting group, adding the reducing matter into uniformly-mixed solution of hydrochloric acid solution and chloralkane; stirring and dissolving clearly; and dipping sodium nitrite solution under a certain temperature to separate out hydrocortisone. With the adoption of the process, the side reaction caused by a large quantity of auxiliary materials during the removal of the protecting group is avoided, so that the product is pure; the production cost is reduced; the hydrocortisone is easily crystallized in heterogeneous solution of the chloralkane and the water; and the crystal form is better than that in the traditional process.

The invention discloses a preparation method of hydrocortisone acetate, belonging to the field of chemical pharmacy. The preparation method comprises the following steps: by using an intermediate Pu's oxide in the traditional cortisone acetate synthesis technique as a raw material, sequentially carrying out ketalation reaction, reduction reaction, hydrolysis reaction, iodine reaction and acetylation reaction under certain conditions to obtain the product hydrocortisone acetate. The preparation method of hydrocortisone acetate has the advantages of accessible raw materials and common auxiliary materials, and does not need some toxic, virulent and cancerigenic reagents in the original technique. The invention is environment-friendly and effective; the product has both high quality and yield; and the HPLC (high performance liquid chromatography) content is up to higher than 98.5%, and the yield is up to higher than 80%.

The invention provides a preparing method of cortisone acetate. The method comprises the three following steps of iodine solution preparation, the iodo reaction and the replacement reaction. In the step one, an idodine solution and bromine are mixed to prepare bromine and iodine liquid. In the step two of the iodo reaction, a reactant 17 alpha-hydroxyl-pregnene-4-alkene-3,11,20-triketone (I) and the bromine and iodine liquid are subjected to the iodo reaction to obtain an intermediate product iodine substitute (II). In the step three of the replacement reaction, the iodine substitute (II) and acetate are subjected to the replacement reaction to obtain a final product cortisone acetate (III). According to the preparing method, the bromine and iodine mixture iodo reaction replaces the traditional iodo reaction, the amount of adopted iodine is reduced greatly, cost is low, environmental pollution is reduced, and applicability is high.

The invention discloses a preparation method of cortisone acetate, which comprises the following steps: preparing the raw material 11-hydroxy-16,17-epoxy-4-ene-3,20-dione into 17-alpha-hydroxy-4-pregnene-3,11,20-trione; and carrying out substitution and replacement reaction on the 17-alpha-hydroxy-4-pregnene-3,11,20-trione with raw materials bromine, potassium acetate and the like to obtain the cortisone acetate. The method specifically comprises the following steps:(a) in an inert gas protective atmosphere, reacting 17-alpha-hydroxy-4-pregnene-3,11,20-trione with pyrrolidine by using alcohol as a solvent to obtain an intermediate compound A; and (b) in an inert gas protective atmosphere and in the presence of catalysts methylsulfonic acid and triethyl orthoformate, carrying out substitution reaction on the intermediate compound A and bromine by using alcohol as a solvent, and carrying out replacement reaction on the product and postassium acetate to obtain the cortisone acetate. The new process disclosed by the invention can greatly lower the production cost of cortisone acetate.

This invention discloses a 6alpha-methylprednisolone and production method of its derivate. This invention uses cortisone acetate and its derivate as raw material to produce 6alpha-methylprednisolone and its derivate. Its production method includes steps such as: lead-in methenyl at sixth position, methenyl is transformed to alpha-methyl, 1,2 position is dehydrogenated to 6alpha-methyl prednisoni acetasby by method of arthrobacterium biotransformation, then selectively hydrogenise 11-ketone to 11 beta-hydroxy group. Using this invention can obtain higher 6alpha-methylprednisolone and yield and quality of its derivate. This invention has characteristics such as: position specificity is high, yield is high. It has important significance for preparing steroid medicine.

The invention relates to the technical field of chemical pharmacy, in particular to a method for treating prednisone acetate mother liquor. The method comprises the following steps: (1) adding a solvent and alkali liquor into the prednisone acetate mother liquor to carry out hydrolysis reaction; (2) after the hydrolysis reaction is finished, adjusting the reaction liquid to be neutral, concentrating under reduced pressure until a large amount of crystals are separated out, and performing suction filtration to obtain a hydrolysate crude product; (3) adding the hydrolysate crude product into a solvent, and refining to obtain a hydrolyzed refined product; (4) adding the hydrolyzed refined substance and a catalyst into a solvent, and reacting with acetic anhydride to obtain a mixture of prednisone acetate and cortisone acetate; and (5) fermenting and dehydrogenating the mixture to obtain the prednisone acetate. According to the treatment method, the prednisone acetate in the prednisone acetate mother liquor can be recycled, particularly, the prednisone acetate in the mother liquor can be recycled, the treatment cost is saved, and the yield of the prednisone acetate is increased; The method can well remove the dehydrogenation RSA and RSA impurities, and is stable in processand simple to operate.

The invention relates to a method for preparing hydrocortisone. The method includes: subjecting a cortisone acetate raw material to sites No. 3,20-keto protective reaction, site No.11-keto reduction reaction, site No.21-hydroxy esterification reaction, sites No. 3,20-ketone deprotection reaction, and site No. 21-acetate hydrolysis to obtain hydrocortisone. The method provides a new synthetic route containing esterification and deprotection in order, greatly improves the reaction selectivity, easily separates deprotection reaction products and avoids the posttreatment of tedious several times of extraction of a large amount of solvents in the traditional deprotection reaction process, and also avoids the side reaction caused by quenching reaction in the posttreatment of the traditional process; and the ester hydrolysis reaction is carried out under protection of inert gases in a mixed solvent, so as to avoid by-products produced in the hydrolysis reaction. The process route of the invention is novel, simple for operation, low in production cost, and applicable to industrial scale production.

The invention discloses a process method for producing an intermediate 3,20-diethylene glycol of betamethasone serial products, which belongs to the field of chemical medicaments. The method comprises the following steps: using a cortisone acetate intermediate prowazekii oxide (1) and glycol as raw materials, boron trifluoride and triethyl orthoformate as catalysts, and chloralkane as a menstruum to perform reaction; and concentrating, crystallizing, filtering, washing and drying the reactants to obtain a reaction product. The method can increase the batch charging concentration, shorten the reaction time, and greatly improve the yield and the quality of a condensation compound. Besides, the method reduces the equipment loss, avoids the use of benzene solvents which are more harmful, and greatly reduces the harm to health and the pollution to the environment.

The invention relates to a recycling method of a cortisone acetate biological catalysis cyclodextrin medium, and belongs to the technical field of biotransformation. The recycling method comprises the following steps of: processing a cyclodextrin-containing transfer solution by filtering and extracting with an organic solvent; removing the residual organic solvent from a cyclodextrin-containing extraction phase; adding to perform biological catalysis of a water repellent compound again, thus realizing the recycle of high-price cyclodextrin as well as environmentally-friendly and clean production of biological catalysis. The recycling method saves the production cost, and has a wide application prospect.

The invention discloses a medicinal composition for treating lung diseases, as well as a preparation method and use of the medicinal composition. The medicinal composition is prepared according to the proportion of carbamide: cortisone acetate: dexamethasone: N-acetyl-cysteine: heparin sodium: sorbitan tri-oleate: 1,1,1,2-tetrafluoroethane: methylparaben of 1:(1-4):(1-3):2:2:2:5:1, and is loaded into an aerosol can with a quantitative aerosol valve to prepare aerosol; active ingredients of the medicinal composition are subjected to freeze drying at first, then are micronized by adopting a high-energy ball mill or jet mill technology, and are loaded into the aerosol can of which the medicament release range of the quantitative aerosol valve is 30 to 250 microliters. The medicinal composition is directly administrated through the lung, so that the utilization rate of the medicinal composition is increased, anti-inflammation and antiviral effects are achieved, and meanwhile, the oxygen absorption of a patient is increased.

The invention relates to a medicament for treating herpes and neurodermatitis, which is prepared from the following components in percentage by weight: 0.2 to 0.6 g of chlorpheniramine maleate, 0.8 to 1.2 g of fosfomycin sodium, 0.01 to 0.02 g of cortisone acetate eye drops, 8 to 12 g of compositus mentholi cream and 8 to 12 g of triamcinolone acetonide acetate and miconazole nitrate and neomycin sulfate cream. The medicament for treating the herpes and the neurodermatitis has the advantages of good treatment effects on herpes, neurodermatitis, beriberi, psoriasis and cutaneous pruritus, quick response and short healing time.

A compound medicine for treating hemicrania is proportionally prepared from aspirin, caffeine, indometacin and cortal.