CAS: 834153-87-6; (R)-4-((2-(5-(2-Fluoro-3-Methoxyphenyl)-3-(2-Fluoro-6-(Trifluoromethyl)Benzyl)-4-Methyl-2,6-Dioxo-3,6-Dihydropyrimidin-1(2H)-yl)-1-Phenylethyl)Amino)Butanoic Acid

上下游产品

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 methyl (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 3-[(2R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-2,4(1H,3H)-pyrimidinedione trifluoroacetate 5-(2-fluoro-3-methoxyphenyl)-1-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-6-methylpyrimidine-2,4(1H,3H)-dione

Methyl (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置于水,Lithium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应生成 恶拉戈利
参考文献: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
标题: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
摘要: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-Dihydro-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.
DOI:10.1021/jm8006454

专利信息

专利号:US-11858901-B2
优先权日:2019-10-30
标 题: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
发明人：BALLETTE ROBERTO; JIMÉNEZ ALONSO OSCAR; GARCÃ?A GARCÃ?A ELENA; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

专利号:US-11840519-B2
优先权日:2019-09-03
标 题 :Process for the synthesis 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-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
发明人：LENNA ROBERTO; FASANA ANDREA; ORTIZ JERRY
权利人:IND CHIMICA SRL
摘要:The present invention 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-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:

专利号:US-2022281829-A1
优先权日:2019-09-03
标题 :Process for the synthesis 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-1(2h)-pyrimidinyl]-1- phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process

专利号:WO-2018224063-A3
优先权日:2017-06-08
标题 :FORMS IN THE SOLID STATE OF ELAGOLIX
发明人：VLASAKOVA RUZENA; CERNA IGOR; OBADALOVA IVA; KREJCIK LUKAS; DAMMER ONDREJ; SVOBODOVA JAROSLAVA; SEMBERA FILIP
权利人:ZENTIVA KS
摘要:The invention relates to novel solid forms of elagolix and its esters, optionally with acids or polymers, their method of preparation and their use. These solid forms are particularly suitable as intermediates for elagolix synthesis or as components of pharmaceutical formulations.

专利号:WO-2021044230-A1
优先权日:2019-09-03
标题: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 intermediates of said process

专利号:ES-2802815-A1
优先权日:2019-07-12
标 题:SALT 3- [2 (R) -AMINO-2-PHENYLETHYL] -5- (2-FLUORO-3-METOXIFENIL) -1- [2-FLUORO-6- (TRIFLUOROMETIL) BENZYL] -6-METHYL-1H -PYRIMIDIN-2,4 (1H, 3H) -DIONA (I) IN SOLID FORM, PROCEDURE FOR ITS PREPARATION AND USE OF THE SAME IN THE SYNTHESIS OF ELAGOLIX