CAS: 1150560-59-0; 5-(2-Fluoro-3-Methoxyphenyl)-1-(2-Fluoro-6-(Trifluoromethyl)Benzyl)-6-Methylpyrimidine-2,4(1H,3H)-Dione

相似化合物

2756307-50-1 2409132-61-0 2749467-58-9

上下游产品

1-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-5-iodo-6-methylpyrimidine-2,4(1H,3H)-dione (2-fluoro-3-methoxyphenyl)boronic acid N-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}urea 5-bromo-6-methyluracil 3-[(2R)-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-2,4(1H,3H)-pyrimidinedione trifluoroacetate 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 4-((R)-2-[5-(2- fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl ]-1- phenylethylamino)-butyric acid (R)-(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)carbamic acid tert-butyl ester

1-[2-氟-6-(三氟甲基)苄基]-5-碘-6-甲基嘧啶-2,4(1H,3H)-二酮置于tris-(Dibenzylideneacetone)Dipalladium(0),甲烷磺酸,三(邻甲基苯基)磷,锌体系中,用 N,N-二甲基乙酰胺,N,N-二甲基甲酰胺 用作溶剂,化学反应 4.0H,反应生成5-(2-氟-3-甲氧基苯基)-1-[[2-氟-6-(三氟甲基)苯基]甲基]-6-甲基-2,4(1H,3H)-嘧啶二酮
参考文献:促性腺激素释放激素拮抗剂中间体及拮抗剂 钠的制备方法
标题:促性腺激素释放激素拮抗剂中间体及拮抗剂 钠的制备方法
摘要:本发明公开了促性腺激素释放激素拮抗剂中间体及拮抗剂钠的制备方法,通过将将化合物1与活性锌在非质子化溶剂中反应得到有机锌试剂,之后进行negishi偶联反应得到目标中间体,进而合成得到促性腺激素释放激素拮抗剂钠.本发明反应条件温和,操作简单,副反应少,降低了制备gnrhr药物的生产质量风险.可以直接"一锅法"制备中间体化合物,中间体易于分离和纯化,操作简单且重现性好,产品纯度和收率高于现有技术.同时本发明的原料安全且成本较低,且绿色环保,有利于控制成本及保护环境.

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-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: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