830346-50-4Relevant academic research and scientific papers
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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, (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.
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 30-36, (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
PROCESS FOR PREPARING ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
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Paragraph 0125; 0126, (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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, (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
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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Page/Page column 11-12, (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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, (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
GnRH receptor antagonist key intermediate and preparation method thereof
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Paragraph 0042; 0047-0048; 0049; 0054-0055, (2020/10/21)
The invention belongs to the technical field of medicines, and particularly relates to a GnRH receptor antagonist key intermediate and a preparation method thereof. The preparation method includes thesteps of enabling a compound 2 and a chiral auxiliary (S)-tert-butylsulfinamide to be subjected to a condensation reaction under the action of a condensing agent to generate an imine compound 3; under the action of a reducing agent, reducing the imine compound 3 obtained in the step (1) to obtain a compound 4; performing acid hydrolysis on the compound 4 to obtain salt of a compound 1, and performing alkali treatment to obtain the compound 1. The chiral auxiliary is introduced to induce chirality, an existing chiral source method is overcome, and the method is easy to operate, mild in condition, good in yield, high in chemical purity and optical purity and suitable for industrial production.
PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND INTERMEDIATES THEREOF
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Page/Page column 27; 30, (2020/10/17)
The present invention relates to compounds of Formula A, isomers, polymorphs and process of preparation thereof, wherein, S is a pharmaceutically acceptable salt, R is selected from hydrogen or C1-C3 alkyl group substituted with Rsu
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.
Intermediate crystal form A of rotigotine and sodium salt thereof as well as preparation method and application thereof (by machine translation)
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Paragraph 0023, (2020/10/04)
The invention discloses an intermediate crystal form A of and a sodium salt thereof, and a preparation method and application thereof, and relates to a medicine intermediate and a preparation method and application thereof. The preparation method provided
