(2-Fluoro-3-Methoxyphenyl)-Dimethoxyborane置于盐酸体系中,化学反应生成2-氟-3-甲氧基苯硼酸 参考文献:Substituted 3-Amino Biaryl Propionic Acids As Potent Vla-4 Antagonists 标题:Substituted 3-Amino Biaryl Propionic Acids As Potent Vla-4 Antagonists 摘要:A Series Of Substituted N-(3,5-Dichlorobenzenesulfonyl)-(L)-Prolyl-And (L)-Azetidyl-Beta-Biaryl Beta-Alanine Derivatives Was Prepared As Selective And Potent Vla-4 Antagonists. The 2,6-Dioxygenated Biaryl Substitution Pattern Is Important For Optimizing Potency. Oral Bioavailability Was Variable And May Be A Result Of Binding To Circulating Plasma Proteins. (C) 2002 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0960-894X(02)00460-2
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:US-2009196912-A1 优先权日:2004-07-30 标 题:Pyridinylamines 发明人:EICKHOFF JAN ELKE; HAFENBRADL DORIS; SCHWAB WILFRIED; COTTON MATTHEW; KIEBL BERT MATTHIAS; ZECH BIRGIT; MULLER STEFAN; HARRIS JOHN; SAVIC VLADIMIR; MACRITCHIE JACKIE 权利人:GPC BOTECH AG 摘要:Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, prion diseases immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.
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: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