- Fulvestrant preparation method
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The invention provides a new fulvestrant synthesis method, which has characteristics of mild reaction condition, simple route and high yield and high purity of each reaction intermediate, can obtain high-purity fulvestrant through re-crystallization without column chromatography, and is suitable for industrial production. The specific technical scheme of the present invention comprises that a compound represented by a formula I and a reagent are subjected to a halogenation reaction in a solvent to generate a compound represented by a formula II; the compound represented by the formula II and thiourea are subjected to a reflux reaction in a solvent to generate a compound represented by a formula III; the compound represented by the formula III and a compound represented by a formula IV aresubjected to a nucleophilic substitution reaction and a hydrolysis reaction in an alkali solution and an organic solvent to generate a compound represented by a formula V; and the compound representedby the formula V is oxidized with an acetic acid hydrogen peroxide oxidation system in a solvent to obtain fulvestrant.
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Paragraph 0119-0120
(2019/10/01)
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- A new compound and its preparation method and elimination method (by machine translation)
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The invention relates to medical and chemical field, provides a new compound, the compounds have the formula I structure, is preparing novel anti-breast cancer drug of fulvestrant in the process more difficult to avoid one of the impurity. The present invention provides a compound of formula I of the synthetic route, and to reduce or avoid the preparation of fluorine Uygursi Qun produced in the process of method, and in its generated after the method of removing it, not only reduces the growing into this impurity the waste of raw materials, also there to have ruled out the impurities to the rear edge of fulvestrant to purification of the product and the impact of the yield. (by machine translation)
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- PROCESS AND INTERMEDIADES FOR THE PREPARATION OF 7-ALKYLATED STEROIDS
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A process for preparing compounds of formula (I), or a salt, solvate or stereoisomer thereof, including Fulvestrant, which process comprises free radical to a compound of formula (III), or a salt, solvate or stereoisomer thereof. The invention also refers to intermediates of said process.
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- Process for the preparation of 7alpha-alkylated 19-norsteroids
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Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.
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Page/Page column 25
(2008/06/13)
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