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
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.
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 catalytically synthesizing elagolix intermediate through organic metal palladium
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, (2019/06/05)
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.
Method for preparing agomelatine intermediate (by machine translation)
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Paragraph 0075; 0098-0100, (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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Paragraph 0140-0142, (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.
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.