832720-84-0Relevant academic research and scientific papers
AN IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM
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Page/Page column 13; 19; 21, (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
PROCESS FOR PREPARING ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
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Paragraph 0127; 0128, (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
3-((R)-2-(AMINO-2-PHENYLETHYL)-1-(2-FLUORO-6-TRIFLUOROMETHYL BENZYL)-5-IODO-6-METHYL-1H-PYRIMIDINE-2,4-DIONE OR A SALT THEREOF, PROCESS FOR ITS PREPARATION, AND ITS USE IN THE SYNTHESIS OF ELAGOLIX
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Page/Page column 36-37, (2021/05/07)
The present invention relates to a new intermediate useful in the synthesis of elagolix, to a process for obtaining said intermediate, to the use of said intermediate for preparing elagolix, and to a process for preparing elagolix making use of said inter
AN IMPROVED PROCESS FOR THE PREPARATION OF 4-({(1 R)-2-[5-(2-FLUORO-3METHOXYPHENYL)-3-{[2-FLUORO-6-(TRIFLUORO METHYL) PHENYL]METHYL}-4-METHYL-2,6-DIOXO-3,6DIHYDROPYRIMIDIN-1(2 H)-YL]-1-PHENYLETHYL}AMINO)BUTANOIC ACID OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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Page/Page column 20, (2021/07/02)
The present invention relates to an improved process for the preparation of 4- ({(1R) -2- [5- (2-fluoro- 3- methoxy phenyl) – 3 - {[ 2-fluoro- 6-(trifluoro methyl) phenyl] methyl} -4-methyl- 2,6-dioxo- 3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino) butanoic acid of formula (I) or its pharmaceutically acceptable salts. The compound of formula (I) is represented by the following structural formula.
Intermediate of Elagolix as well as preparation method and application of intermediate
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, (2021/11/26)
The invention provides a novel method for preparing a key intermediate 1 of Elagolix, and provides several novel intermediate compounds at the same time. Through the novel intermediate and the preparation method, the raw material and synthesis cost is greatly reduced, and the yield is also greatly improved. Meanwhile, the intermediate is low in reaction energy consumption, few in 'three wastes', mild in reaction condition and easier for industrial large-scale production.
Preparation method of oxragolian sodium
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, (2021/04/21)
The invention provides a preparation method of oxagolide sodium. According to the method, the synthetic route of the oxogoliride sodium is improved, Boc protecting groups are removed by using concentrated hydrochloric acid, and then the oxogoliride sodium
PROCESS FOR THE SYNTHESIS OF THE SODIUM SALT OF 4-[[(LR)-2-[5-(2-FLUORO-3-METHOXYPHENYL)-3-[[2-FLUORO-6-(TRIFLUOROMETHYL)-PHENYL]METHYL]-3,6-DIHYDRO-4-METHYL-2,6-DIOXO-L(2H)-PYRIMIDINYL]-L- PHENYLETHYL]AMINO]-BUTANOIC ACID (ELAGOLIX SODIUM SALT) AND INTER
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, (2021/03/13)
The present invention relates to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-l(2H)-pyrimidinyl]-l-phenylethyl]-amino]-butanoic a
Preparation method of elagolix sodium and intermediate thereof
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Paragraph 0061; 0068; 0069; 0070; 0071; 0072; 0073, (2021/03/11)
The invention relates to a preparation method of elagolix sodium and an intermediate thereof, and relates to the technical field of medicine synthesis and preparation. The preparation method comprisesthe following synthesis steps: (1) synthesizing a compound 2 by taking D-phenyl glycinol 1 and ethyl 4-bromobutyrate as raw materials through a substitution reaction; (2) reacting with a compound 3 to generate a compound 4; and (3) salifying to obtain a target product 5, namely elagolix sodium. The preparation method disclosed by the invention has the characteristics of suitability for industrialproduction, lower cost, high purity of the prepared product and high yield.
3-[2(R)-AMINO-2-PHENYLETHYL]-5-(2-FLUORO-3-METHOXYPHENYL)-1-[2-FLUORO-6-(TRIFLUOROMETHYL)BENZYL]-6-METHYL-1H-PYRIMIDINE-2,4(1H,3H)-DIONE HYDROCHLORIDE SALT (I) IN SOLID FORM, PROCESS FOR PREPARING SAME, AND USE THEREOF IN THE SYNTHESIS OF ELAGOLIX
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, (2021/02/12)
The present invention relates to a new intermediate useful in the synthesis of elagolix, to a process for obtaining same, to the use of said intermediate for preparing elagolix, and to a process for preparing elagolix making use of said intermediate.
IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES
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Page/Page column 23; 27-28, (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
