CAS: 239087-06-0; 2-Fluoro-6-(Trifluoromethyl)Benzylamine

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CAS号133116-83-3 2-氟-6-(三氟甲基)苯甲腈 | CAS号830346-46-8 1-[2-氟-6-(三氟甲基)苄基]脲

在 肼体系中,用 乙醇 用作溶剂,化学反应 1.5H,以85%的收率获得2-氯-6-(三氟甲基)苄胺
参考文献:一种elagolix中间体2-氟-6-三氟甲基苄胺的制备方法
标题:一种elagolix中间体2-氟-6-三氟甲基苄胺的制备方法
摘要:本发明公开了一种elagolix中间体2‑氟‑6‑三氟甲基苄胺的制备方法,属于医药中间体技术领域.它包括以下步骤:(1)2‑氟‑6‑(三氟甲基)苯甲酸的合成;(2)2‑氟‑6‑(三氟甲基)苯甲醇的合成;(3)2‑氟‑6‑(三氟甲基)苯甲磺酸酯,邻苯二甲酰亚胺化合物的合成;(4)邻苯二甲酰亚胺化合物直接合成;(5)2‑氟‑6‑三氟甲基苄胺的合成.该制备方法通过对反应试剂,反应的溶剂等因素进行了优化,使得反应条件温和,工艺流程简便,对设备的要求比较低,原料价格也更加便宜,所得到产物得纯度高,有利于工业化生产.

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: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: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

专利号:US-2023025807-A1
优先权日:2019-10-30
标题:Cd38 inhibitors
发明人：KULKARNI SANTOSH S; LAGU BHARAT; WU XINYUAN
权利人:MITOBRIDGE INC
摘要:The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD + or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).