830346-51-5

Usage

Uses

Used in Pharmaceutical Industry:
tert-butyl N-[(1R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxo-pyrimidin-1-yl]-1-phenyl-ethyl]carbamate is used as an intermediate in the synthesis of Elagolix-d6 Sodium Salt (E501016), a labelled analogue of Elagolix Sodium Salt (E501018). Elagolix Sodium Salt is a novel uracil phenylethylamine that acts as a potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonist. This antagonistic activity makes it a potential candidate for the treatment of various hormonal disorders and conditions related to the gonadotropin-releasing hormone system.
Used in Research and Development:
Due to its unique structure and potential biological activity, tert-butyl N-[(1R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxo-pyrimidin-1-yl]-1-phenyl-ethyl]carbamate may also be used in research and development for the discovery of new drugs and therapeutic agents. Its synthesis and modification can provide valuable insights into the structure-activity relationships of hGnRH-R antagonists and other related compounds, potentially leading to the development of more effective and targeted treatments for various medical conditions.

Upstream product

• 1150560-59-0 5-(2-fluoro-3-methoxyphenyl)-1-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-6-methylpyrimidine-2,4(1H,3H)-dione 
• 126610-77-3 (R)-tert-butyl N-<1-phenyl-2-<(p-toluenesulfonyl)oxy>ethyl>carbamate 
• 102089-75-8 (-)-(1R)-1-[(1',1'-dimethylethoxycarbonyl)amino]-2-(methylsulfonyl)oxy-1-phenylethane 
• 830346-48-0 5-bromo-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methylpyrimidine-2,4-(1H,3H)-dione 
• 830346-46-8 N-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}urea 
• 239087-06-0 (2-fluoro-6-(trifluoromethyl) phenyl)methanamine 
• 295376-21-5 2-fluoro-3-methoxy-1-bromobenzene 
• 1080673-30-8 2-fluoro-1-iodo-3-methoxybenzene 
• 67341-01-9 (R)-N-(tert-butoxycarbonyl)phenylglycinol 
• 137102-65-9 (R)-(2-amino-1-phenyl-ethyl)-carbamic acid tert-butyl ester 
• 134364-69-5 2.3-difluoroanisole 
• 830346-47-9 1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-2,4(1H,3H)-pyrimidinedione 
• 352303-67-4 (2-fluoro-3-methoxyphenyl)boronic acid 
• 15018-56-1 5-bromo-6-methyluracil 

Downstream Products

• 1092071-03-8 3-[(2R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-2,4(1H,3H)-pyrimidinedione trifluoroacetate 
• 832720-84-0 4-((R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidine-1-yl]-1-phenylethylamino)butyric acid ethyl ester 
• 830346-50-4 3-[(2R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-2,4(1H,3H)-pyrimidinedione trifluoroacetate 

Relevant 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

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.

Preparation method of oxragolian sodium

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

AN IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM

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

Substituted pyrimidine-2, 4(1H, 3H)-dione derivative and uses thereof

The invention belongs to the technical field of medicines, and relates to a substituted pyrimidine-2, 4(1H, 3H)-dione derivative and uses thereof, and a pharmaceutical composition containing the compound. The derivative and the pharmaceutical composition can be used as gonadotropin releasing hormone receptor antagonists. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and uses of the compound and the pharmaceutical composition in prevention or treatment of sex hormone dependent diseases including but not limited to prostate cancer, endometriosis, hysteromyoma, precocious puberty and the like.

PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND INTERMEDIATES THEREOF

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

Intermediate crystal form A of rotigotine and sodium salt thereof as well as preparation method and application thereof (by machine translation)

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

IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES

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

Preparation method of gonadotropin releasing hormone antagonist

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.

PROCESS FOR PREPARING ELAGOLIX

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.

Method for catalytically synthesizing elagolix intermediate through organic metal palladium

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.