1150560-59-0Relevant articles and documents
PROCESS FOR PREPARING ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
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Paragraph 0119; 0120, (2021/03/19)
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
AN IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM
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Page/Page column 13; 18; 19-20, (2021/04/10)
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
Elagolix Sodium Compositions and Processes
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Paragraph 0429, (2020/02/13)
The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.
IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES
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Paragraph 25-26, (2020/12/11)
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
Synthesis method of elagolix intermediate
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, (2020/02/17)
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.
Method for preparing elagolix intermediate
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, (2020/01/25)
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.
PROCESSES TO PRODUCE ELAGOLIX
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Page/Page column 14, (2019/06/23)
The present invention relates to a scalable process for the making of elagolix, its salts and the process of intermediate compounds.
Method for preparing agomelatine intermediate (by machine translation)
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, (2019/12/09)
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)
Method for preparing intermediate of elagolix
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, (2019/12/09)
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.
Preparation method of gonadotropin releasing hormone antagonist intermediate and sodium antagonist
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, (2019/11/20)
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.