CAS: 832720-36-2; Sodium,4-[[(1R)-2-[5-(2-Fluoro-3-Methoxyphenyl)-3-[[2-Fluoro-6-(Trifluoromethyl)Phenyl]Methyl]-4-Methyl-2,6-Dioxopyrimidin-1-Yl]-1-Phenylethyl]Amino]Butanoate

恶拉戈利 反应生成 恶拉戈利钠
参考文献: Pyrimidine-2,4-Dione Derivatives As Gonadotropin-Releasing Hormone Receptor Antagonists[fr] Derives De Pyrimidine-2,4-Dione Utilises Comme Antagonistes Du Recepteur D'Hormone Liberant De La Gonadotrophine
标题: Pyrimidine-2,4-Dione Derivatives As Gonadotropin-Releasing Hormone Receptor Antagonists[fr] Derives De Pyrimidine-2,4-Dione Utilises Comme Antagonistes Du Recepteur D'Hormone Liberant De La Gonadotrophine
摘要:Gnrh受体拮抗剂被披露,对男性和女性的各种与性激素相关的疾病具有治疗作用.本发明的化合物具有以下结构:其中r1A,R1B,R1C,R2A,R2B,R3,R4,R5,R6和x的定义如本文所述,包括立体异构体,前药和其药用可接受盐.还披露了含有本发明化合物的组合物与药用可接受载体的组合物,以及与在需要时对抗性腺激素释放激素的使用方法.

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: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

专利号:CA-3149179-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:US-2022411382-A1
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