合成目标产物 1-(2-Fluoro-6-(Trifluoromethyl)Benzyl)-6-Methylpyrimidine-2,4(1H,3H)-Dione 主要起始原料 6-Methyluracil And 2-Fluoro-6-(Trifluoromethyl)Benzyl Bromide
239087-06-0 + 57-13-6 = 830346-47-9 反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Water; Reflux2.1 Solvents: Toluene; Reflux2.2 Reagents: P-Toluenesulfonic Acid; Reflux 标题:Elagolix Sodium Salt And Its Synthetic Intermediates: A Spectroscopic,Crystallographic,And Conformational Study 作者:Ciceri,Samuele; Et Al 参考文献:Molecules 日期:2023 卷标:28(9)]
830346-46-8 = 830346-47-9 反应条件:1.1 Reagents: Chlorotrimethylsilane,Sodium Iodide Solvents: Acetonitrile; 0 °C; 0 °C -> Rt; 20 H,Rt 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 作者:Chen,Chen; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2008 卷标:51(23) 页码:7478-7485]
830346-46-8 + 1694-31-1 = 830346-47-9 反应条件:1.1 Solvents: Toluene; Reflux1.2 Reagents: P-Toluenesulfonic Acid; Reflux 标题:Elagolix Sodium Salt And Its Synthetic Intermediates: A Spectroscopic,Crystallographic,And Conformational Study 作者:Ciceri,Samuele; Et Al 参考文献:Molecules 日期:2023 卷标:28(9)
2-氟-6-(三氟甲基)苯甲醛置于盐酸,盐酸羟胺,氢气,碳酸氢钠,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,乙醇,水,N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,15.0~130.0 °C,300.01 Kpa 条件下,反应 14.0H,反应生成 1-[2-氟-6-(三氟甲基)苄基]-6-甲基嘧啶-2,4(1H,3H)-二酮 参考文献: Processes To Produce Elagolix[fr] Processus De Production D'élagolix 标题: Processes To Produce Elagolix[fr] Processus De Production D'élagolix 摘要:本发明涉及一种用于制备依诺司特及其盐和中间化合物的可扩展工艺.
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-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
专利号:ES-2822398-A1 优先权日:2019-10-30 标 题 :3 - ((R) -2- (Amino-2-phenylethyl) -1- (2-fluoro-6-trifluoromethylbenzyl) -5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt of the same, procedure for its preparation and its use in the synthesis of elagolix
专利号:ES-2822398-B2 优先权日:2019-10-30 标 题:3-((R)-2-(Amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidin-2,4-dione or a salt of the same, procedure for its preparation and its use in the synthesis of elagolix
专利号:WO-2021083554-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