- X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain
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An X-ray crystal structure is reported for the novel enhanced-affinity glucocorticoid agonist fluticasone furoate (FF) in the ligand binding domain of the glucocorticoid receptor. Comparison of this structure with those of dexamethasone and fluticasone pr
- Biggadike, Keith,Bledsoe, Randy K.,Hassell, Anne M.,Kirk, Barrie E.,McLay, Iain M.,Shewchuk, Lisa M.,Stewart, Eugene L.
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- A method for preparing pyromucic acid fluorine for kasong (by machine translation)
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The present invention provides a method for preparing pyromucic acid fluorine for kasong, comprises the following steps: 1) compound VIII in alkali and alcohol solvent in the presence of a hydrolysis to obtain compound II; 2) compound II in reductive salt as catalyst under the condition be, pyromucic acid fluorine for kasong fluorine halogen reaction with methane (compound I). The present invention in order to have the reducing inorganic salt as a catalyst, greatly reducing disulfide impurity, mercapto oxide impurity, and mercapto oxide introduced [...] formation of impurities. (by machine translation)
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Paragraph 0049; 0050
(2019/10/22)
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- Preparation method of fluticasone furoate
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The invention relates to a preparation method of fluticasone furoate, especially preparation and purification of an intermediate 6alpha, 9alpha-difluoro-17alpha-[(2-furylcarbonyl)oxy]-11beta-hydroxy-16alpha-methyl-3-oxo-androstane-1,4-diene-17beta-thiocarboxylic acid. The preparation method comprises the following steps: in the presence of alkali and alcoholic solvent, a compound as shown in the formula VIII is converted into a mixture containing the compound of formula II; the mixture containing the compound of formula II is mixed with an aqueous solution of inorganic base and an ester solvent; a water phase is separated; pH value of the water phase is regulated by the use of acid until a solid is precipitated out; and the solid is separated. The invention provides a preparation method capable of remarkably raising purity of fluticasone furoate. Safety of drug application is guaranteed.
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- Method for the Production of Fluoromethyl Esters of Androstan-17 beta Carboxylic Acids
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Described herein are processes for the preparation of monofluoromethylated organic biologically active compounds, starting from protected intermediates and/or reagents to obtain compounds such as fluticasone propionate and fluticasone furoate, in presence of decarboxylating reagents XeF2 and BrF3, or using FCH2SH as a reagent.
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- PROCESS FOR PREPARING FLUTICASONE PROPIONATE/FUROATE
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The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.
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- METHOD FOR PREPARING FLUTICASONE FUROATE
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Method for preparing fluticasone furoate (6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-[(2-furoyl)oxy]-3-oxo-androsta-1,4-diene-17β-carbothioic acid S-fluoromethyl ester) by directly subjecting a compound of Formula III and a complex of a fluoromethylating reagent in presence of an organic base to a replacement reaction to obtain the target compound. Generation of impurities in a process via Compound IV is avoided; the method is simple with mild reaction conditions, suitable for industrial production, and yields products with purity of 98% by HPLC.
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- METHOD FOR THE PRODUCTION OF FLUOROMETHYL - ESTERS OF ANDROSTAN- 17 - BETA - CARBOXYLIC ACIDS
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The present invention relates to a method of preparing an organic biologically active compound of formula (I), wherein R1, R2, R3, R4,. X1, X2 and X3 are as defined in the specification, to certain novel intermediates obtainable from such a method and their use.
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Page/Page column 17
(2012/12/13)
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- METHODS AND COMPOUNDS FOR THE PREPARATION OF MONOFLUOROMETHYLATED BIOLOGICALLY ACTIVE ORGANIC COMPOUNDS
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The present invention describes processes for the preparation of, monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such as XeF2 and BrF3.
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Page/Page column 7
(2011/12/14)
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- METHOD FOR MONOFLUOROMETHYLATION OF ORGANIC SUBSTRATES TO PREPARE BIOLOGICALLY ACTIVE ORGANIC COMPOUNDS
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The present invention describes a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5- tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.
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Page/Page column 8
(2011/12/14)
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- POLYMORPHS OF FLUTICASONE FUROATE AND PROCESS FOR PREPARATION THEREOF
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Provided are polymorphs of fluticasone furoate and processes for preparation thereof.
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Page/Page column 26
(2010/04/03)
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- Process for the Preparation of 6-alpha,9-alpha-difluoro-17-alpha-((2-furanylcarbonyl)oxy)-11-beta-hydroxy-16-alpha-methyl-3-oxo-androsta-1,4-diene-17-beta- -carbothioic acid S-fluoromethyl
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A novel process for preparing a compound of formula (I) which comprises converting a compound of formula (II) to a compound of formula (I) via a compound of formula (III), or a salt thereof, without isolating any intermediates.
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Page/Page column 4
(2009/05/28)
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- Pharmaceutical formulation comprising an androstane derivative and a solubilising agent in an aqueous liquid carrier
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A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I) wherein R represents a 5 membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O, N and S, optionally substituted by one or more methyl or halogen atoms or a solvate thereof, as a medicament; and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.
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- Anti-inflammatory androstane derivative compositions
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There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121having unit cell dimensions of about 12.1±0.6 ?, 14.9±0.7 ?, and 16.2±0.8 ? when determined at either 120K or 150K.
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- Anti-inflammatory androstane derivative compositions
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There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212121having unit cell dimensions of about 7.6±0.6 ?, 12.7±0.7 ?, and 33±3 ? when determined at 120K.
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- Novel anti-inflammatory androstane derivative compositions
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There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212121 having unit cell dimensions of about 7.6±0.6 ?, 12.7±0.7 ?, and 33±3 ? when determined at 120K.
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- Novel anti-inflammatory androstane derivative compositions
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There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 12.1±0.6 ?, 14.9±0.7 ?, and 16.2±0.8 ? when determined at either 120K or 150K.
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