- Intermediate of Elagolix as well as preparation method and application of intermediate
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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.
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- 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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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.
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- 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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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
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- Preparation method of oxragolian sodium
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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
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- 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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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
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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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- Preparation method of elagolix sodium and intermediate thereof
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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.
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Paragraph 0061; 0068; 0069; 0070; 0071; 0072; 0073
(2021/03/11)
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- 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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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.
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- 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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- 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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- 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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- 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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- Preparation method of gonadotropin releasing hormone antagonist
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The invention discloses a preparation method of a gonadotropin releasing hormone antagonist. According to the preparation method of the gonadotropin releasing hormone antagonist, a synthesis route ofNBI-56418 sodium is changed, an organic zinc reagent is used as a coupling reagent to perform a Negishi coupling reaction, conditions are mild and easy to control, few steps are performed, the reproducibility is good, the total yield is greatly improved, and the product purity is high and reaches more than 98.5%; and meanwhile, raw materials of the synthesis method are safe and low in cost and areenvironmentally friendly, and large-scale production is facilitated. If organic acid or mineral acid is added for activation during the preparation of the organic zinc reagent, the obtained organic zinc reagent can enable the activity of the Negishi coupling reaction to be higher, and the yield, the total yield and the product purity are further improved. According to the preparation method, hydrochloric acid is adopted to remove Boc, the cost is reduced, and side reactions can further be effectively reduced.
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- PROCESS FOR PREPARING ELAGOLIX
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The application relates to a process for the preparation of compound of formula (1) or a salt thereof (i.e. elagolix): The application also relates to solid crystalline forms of intermediates used in the process.
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- A multi-substituted pyrimidine derivatives of synthetic method
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The present invention discloses a multi-substituted pyrimidine derivatives of the synthetic method, the formula II shown in the (R)- 3 - (2 - amino - 2 - phenethyl) - 5 - (2 - fluoro - 3 - methoxyphenyl) - 1 - (2 - fluoro - 6 - (trifluoromethyl) benzyl) -
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Paragraph 0022-0034
(2019/06/05)
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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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- PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND ITS POLYMORPH
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The present invention provides a process for preparation of Elagolix and its intermediates, processes for preparation of amorphous Elagolix sodium and solid dispersion of Elagolix Sodium thereof.
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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 17-20
(2009/06/27)
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- Discovery of sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6- [trifluoromethyl]-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl] -1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor
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The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonists is described. A major focus of this optimization was to improve the CYP3A4 inhibition liability of these uracils while maintaining their GnRH-R potency. R-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl) -4-methyl-2,6-dioxo-3,6-dihy-dro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyric acid sodium salt, 10b (elagolix), was identified as a potent and selective hGnRH-R antagonist. Oral administration of 10b suppressed luteinizing hormone in castrated macaques. These efforts led to the identification of 10b as a clinical compound for the treatment of endometriosis.
- Chen, Chen,Wu, Dongpei,Guo, Zhiqiang,Xie, Qiu,Reinhart, Greg J.,Madan, Ajay,Wen, Jenny,Chen, Takung,Huang, Charles Q.,Chen, Mi,Chen, Yongsheng,Tucci, Fabio C.,Rowbottom, Martin,Pontillo, Joseph,Zhu, Yun-Fei,Wade, Warren,Saunders, John,Bozigian, Haig,Struthers, R. Scott
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experimental part
p. 7478 - 7485
(2009/12/07)
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- PYRIMIDINE-2, 4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS
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GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
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