- Fluorometholone, fluorometholone acetate, and preparation method thereof
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The invention discloses fluorometholone, fluorometholone acetate, and a preparation method thereof. According to the preparation method, a compound represented by a formula (II) is taken as a raw material, the compound carries out de-chlorination reaction, esterification reaction, methenylation reaction, hydrogenation reaction, fermentation de-hydrogenation reaction, epoxidation reaction, and ring-opening reaction in sequence to obtain derivatives of fluorometholone; and fluorometholone derivatives carry out hydrolysis to obtain fluorometholone. The preparation method has the advantages of short synthesis route, high yield, low raw material cost, easily available raw materials, simple and convenient purification, high product purity, and strong technological operability, is suitable for industrial production, and has a high industrialization value.
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Paragraph 0069-0075
(2020/03/12)
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- Synthesis method and application of 9-fluorosteroid compound
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The invention provides a synthesis method and application of a 9-fluorosteroid compound, and relates to the technical field of chemical synthesis. The synthesis method of the 9-fluorosteroid compoundcomprises the following step: reacting a compound II in an ionic liquid containing hydrogen fluoride salt to obtain a 9-fluorosteroid compound III. According to the synthesis method of the 9-fluorosteroid compound, the ionic liquid containing the hydrogen fluoride salt is used as a fluorinating agent to replace a traditional hydrogen fluoride aqueous solution, volatilization of hydrogen fluoride gas is avoided, corrosivity is small, toxicity is greatly reduced, reaction conditions are mild, reaction can be completed at the room temperature, operability is high, the safety coefficient is high,and production applicability is improved. The synthesis method of the 9-fluorosteroid compound is used for preparing corticosteroid drugs, highly toxic chemical reagents are not used in the synthesisroute, the operability is high, the safety coefficient is high, and the production applicability is improved.
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Paragraph 0089-0096; 0125-0127
(2021/01/15)
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- Sterides ring expanding compound and preparation method thereof
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The invention provides a sterides ring expanding compound which is characterized by having a structure shown as a formula I shown in the accompanying drawing or being enantiomers, or solvates or aquo-complexes of the compound with the formula I. The sterides ring expanding compound has the advantages and positive effects that the compound with the formula I can be effectively combined with glucocorticoid receptors; the pharmacological effects identical to glucocorticoid can be generated; the toxicity is lower than that of the glucocorticoid.
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Paragraph 0034; 0039; 0044; 0048; 0052
(2019/10/15)
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- PROCESS FOR OBTAINING FLUOROMETHOLONE AND INTERMEDIATES THEREFOR
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The present invention relates to a process for obtaining compounds of formula (I) and (V), wherein R1 is C1-C6 alkyl; and R2 is OR3, OC(=O)R4 or O-(HPG), wherein R3 is H, C1-C6 alkyl or C6-C14 aryl; R4 is H or C1-C6 alkyl; and HPG is a hydro xyl protecting group, intermediates useful in the synthesis of some steroids, for example, fluorometholone and derivatives thereof. The invention also relates to other intermediates useful in synthesis.
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Page/Page column 29
(2010/11/05)
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- Chemoselective hydrogenation of 17α-hydroxy-6-methylen-pregna-4,9(11)-diene-3,20-dione. Synthesis of fluorometholone
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The development of an efficient hydrogenation method of 17α-hydroxy-6-methylen-pregna-4,9(11)-diene-3,20-dione by using wet (10%) Pd on carbon and triethylamine led us to the corresponding 6α-methyl-pregnane in good yield. This chemoselective process allo
- Marcos-Escribano, Andrés,Bermejo, Francisco A.,Bonde-Larsen, Antonio Lorente,Retuerto, Jesús Iglesias
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experimental part
p. 8493 - 8496
(2010/01/06)
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- Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
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Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.
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- Water-soluble steroid compounds
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Beta-cyclodextrin forms a water-soluble complex or inclusion compound with steroid compounds having a molecular structure smaller than the interior cavity in the doughnut-shaped molecular structure of beta-cyclodextrin. The resulting inclusion compounds can be used for a variety of applications including aqueous topical ophthalmic preparations and topical dermatological ointments.
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- Base catalyzed acylation with enol esters
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This invention relates to processes for base catalyzed acylations using enol esters, for example, isopropenyl acetate. Particularly, the processes are useful for acylating acid sensitive alcohols including hydroxy steroids.
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