CAS: 1632006-28-0; 1-(2-Hydroxyethyl)-4-Methyl-N-(4-(Methylsulfonyl)Phenyl)-5-(2-(Trifluoromethyl)Phenyl)-1H-Pyrrole-3-Carboxamide

上下游产品

4-Methyl-N-[4-(Methylsulfonyl)Phenyl]-5-[2-(Trifluoromethyl)-Phenyl]-1H-Pyrrole-3-Carboxamide 880779-74-8
1-(2-Hydroxyethyl)-4-Methyl-5-[2-(Trifluoromethyl)Phenyl]-1H-Pyrrole-3-Carboxylic Acid
Ethyl (Rs)-2-Chloro-1-(2-Hydroxyethyl)-4-Methyl-5-[2-(Trifluoromethyl)Phenyl]-1H-Pyrrole-3-Carboxylate

2'-(三氟甲基)苯丙酮置于吡啶,盐酸,4-二甲氨基吡啶,氯化亚砜,硫酸,5%-Palladium/activated Carbon,水,溴,Sodium Formate,Potassium Carbonate,Potassium Hydroxide,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,甲基叔丁基醚,N,N-二甲基乙酰胺,水,乙酸乙酯,甲苯,乙腈 用作溶剂,化学反应 45.0H,反应生成艾沙利酮
参考文献:Crystal Of Pyrrole Derivative And Method For Producing The Same
标题:Crystal Of Pyrrole Derivative And Method For Producing The Same
摘要:本发明提供了一种具有优异的矿物皮质激素受体拮抗活性的吡咯衍生物的异构体的生产中间体,以及生产该中间体的方法和其晶体.一种生产吡咯衍生物的异构体的方法,包括将由下述一般式(I)表示的化合物(其中r1代表甲基基团或三氟甲基基团,R2代表氢原子或c1-C3烷氧基团,N代表从1到3中选择的整数)分解成其异构体的步骤,其特征在于使用具有奎宁骨架式的光学活性胺,并且晶体为(S)-1-(2-羟乙基)-4-甲基-N-[4-(甲磺基)苯基]-5-[2-(三氟甲基)苯基]-1H-吡咯-3-羧酰胺.

专利信息

专利号:WO-2023035571-A1
优先权日:2021-09-10
标 题:Synthesis method for esaxerenone and intermediate thereof
发明人：RUAN JING; ZHANG XINXIN; YAN GONGCHAO; RUAN XIAONA; ZHANG WEI
权利人:SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD
摘要:Provided is a new synthesis method for an intermediate of esaxerenone. The method comprises: (1) reacting 2-(trifluoromethyl)phenylacetic acid as a raw material with ethyl chloroformate or isobutyl chloroformate in an inert solvent in the presence of an alkali to produce a mixed anhydride, then reacting same with ammonia to obtain a corresponding amide compound of formula II; (2) subjecting the amide compound of formula II obtained in step (1) to a dehydration reaction in the presence of a dehydrating agent and an acid-binding agent to obtain an isocyanide compound of formula III; and (3) subjecting the isocyanide compound of formula III obtained in step (2) to a cyclization reaction with ethyl 2-butynonate in the presence of an alkali and a metal catalyst to form a pyrrole ring compound of formula IV; and the reaction equation is shown below: Compared to the prior art, the technical solution of the present invention has the advantages of a high yield, a simple post-treatment, low costs and easy industrialization, etc.