- PROCESS FOR PREPARING ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
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The present invention provides improved processes for the preparation of elagolix and intermediates thereof. The intermediate of formula VII is achieved by a coupling reaction of a compound of formula V and a N-benzylidene protected compound of formula IV
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- AN IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM
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An improved process for the preparation of Elagolix Sodium having the structural formula (I). The present invention relates to highly pure compound of formula (VI) as a solid which is useful in the preparation of Elagolix sodium. The present invention pro
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Page/Page column 13; 18; 19-20
(2021/04/10)
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- Method for preparing elagolix intermediate
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The invention discloses a method for preparing elagolix intermediate, which is characterized in that it is prepared according to the following steps: 1) subjecting 2-fluorine-3-methoxybromobenzene andethyl acetoacetate to coupling reaction under the action of copper catalyst and L-proline to obtain a compound I, 2) subjecting the compound I and urea to coupling cyclization reaction in the presence of p-toluenesulfonic acid to obtain a compound II, wherein the molar ratio of p-toluenesulfonic acid to compound I is 0.05-0.1:1, 3) reacting that compound II with 2-fluorine-6-trifluoromethyl benzyl bromide to obtain a product. The coupling cyclization reaction is easy, the yield is high, and the consumption of raw materials is low.
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- IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES
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The present invention provides an improved process for the preparation of Elagolix sodium of formula (I) and its intermediates. The present invention also provides a compounds of formula (V) and (VI), (X), (Xa) and (Xb). The present invention further prov
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Paragraph 25-26
(2020/12/11)
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- Synthesis method of elagolix intermediate
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The invention relates to a synthesis method of an elagolix intermediate. Specifically, the invention provides a synthesis method of an elagolix intermediate compound X and an elagolix intermediate compound I. According to the method, 2-fluoro-3-methoxy-phenylacetic acid is used as a raw material, and the steps of cyclization, hydrolysis, amino protection, condensation, Mitsunobu reaction and the like are carried out in sequence, so that the elagolix intermediate compound X and the elagolix intermediate compound I are obtained. The method has the advantages of cheap and easily available reagents, high conversion rate, simple operation and low process cost, and is suitable for industrialization.
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- Elagolix Sodium Compositions and Processes
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The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.
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Paragraph 0429
(2020/02/13)
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- Method for catalytically synthesizing elagolix intermediate through organic metal palladium
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The invention discloses a method for catalytically synthesizing an elagolix intermediate through organic metal palladium. The structure of the elagolix intermediate is as shown in a formula I which isshown in the description; a synthesis route of a compound as shown in the formula I is as shown in the description. The method specifically comprises the steps of synthesis of a compound as shown ina formula VIII, synthesis of a compound as shown in a formula X and synthesis of a final product. Through a synthesis scheme disclosed by the invention, not only synthesis raw materials are cheap andeasy to obtain, the synthesis route is green and environment-friendly, the synthesis steps are less, the yield is high, the production period is short, and the synthesis route is suitable for being used as an industrial production technique route.
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- Method for preparing agomelatine intermediate (by machine translation)
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The invention relates to a method for preparing an intermediate of agomelatine. The method is simple and convenient to E8 operate, mild E8 in condition and very suitable for industrial production C. (by machine translation)
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Paragraph 0075; 0098-0100
(2019/12/09)
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- Method for preparing intermediate of elagolix
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The invention relates to a method for preparing an intermediate of elagolix. In particular, the invention discloses a method for preparing a key intermediate compound E8 of elagolix, and compounds such as a compound E4 for preparing the intermediate compound E8. The method is simple and convenient in operation, mild in condition and very applicable to industrial production.
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Paragraph 0140-0142
(2019/12/09)
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- Preparation method of gonadotropin releasing hormone antagonist intermediate and sodium antagonist
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The invention discloses a preparation method of a gonadotropin releasing hormone antagonist intermediate and sodium antagonist. The preparation method comprises the steps: performing a reaction on a compound 1 and active zinc in a non-protic solvent so as to obtain an organic zinc reagent, then performing a Negishi coupling reaction so as to obtain the target intermediate, and further performing synthesis so as to obtain the gonadotropin releasing hormone antagonist sodium. The preparation method has mild reaction conditions, simple operation and few side reactions, and the risks of productionquality for preparation of GnRHR drugs are reduced; the intermediate compound can be directly prepared by using a one-pot method, the intermediate has easy separation and purification, the operationis simple, the reproducibility is good, and the product purity and yield are higher than the prior art; and meanwhile, the raw materials have safety and low cost, and are environmentally friendly, andcontrol on the cost and protection of the environment are facilitated.
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- PROCESSES TO PRODUCE ELAGOLIX
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The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.
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- Elagolix synthesis method
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The invention provides an elagolix synthesis method. The elagolix synthesis method comprises enabling a compound 5 and a compound 10 to participate in a condensation reaction to finish N-alkylation reaction to obtain a compound 11, and then implementing alkaline hydrolysis to obtain elagolix 12. The invention further discloses two synthesis methods of the compound 5: the method I comprises enabling a 5-bromine-6-methylpyrimidine-2,4(1H,3H)-diketone compound 1 and a 2-(brooethyl)-1-fluorin-3-(trifluoromethyl) benzene compound 2 to have a condensation reaction to obtain an intermediate 3, and then having a coupling reaction; the method II comprises enabling 1-halide-3-fluorin-2-anisole and acetoacetate 7 to have a coupling reaction to obtain a compound 8, and then having a condensation cyclization reaction with a compound 9; the improvements greatly shorten the route steps, the route efficiency is improved, the use of a noble metal catalyst is avoided, and the process cost is greatly lowered. The operation of the route is simple, the total yield is high, the purity of an obtained product is also relatively high, and the method is suitable for the enlarged production.
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- PROCESS FOR THE PREPARATION OF ELAGOLIX AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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The present invention relates to a process for the preparation of Elagolix of formula (I) and its pharmaceutically acceptable salts. The present invention also relates to an intermediate of formula (VIII) and its use in preparation of Elagolix and its pharmaceutically acceptable salts.
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- Deuterated elagolix derivative and use thereof
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The invention discloses a method for preparing a deuterated elagolix derivative. When being used as a GnRH receptor antagonist, the deuterated elagolix derivative has the use of treating disease states relevant to male and female sex hormone. The invention also discloses a composition containing the compound combined with a medicine acceptable carrier, and a method for antagonizing intraindividualgonadotropin to release hormone by using the composition.
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Paragraph 0037; 0039; 0040
(2018/07/06)
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- PROCESSES FOR THE PREPARATION OF URACIL DERIVATIVES
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The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
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Page/Page column 8-10
(2009/06/27)
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