Efletirizine, Ucb-28754
乙氟利嗪 醋酸,2-[2-[4-[双苯甲基(4-氟苯基)甲基]-1-哌拉嗪基]乙氧基]-,盐酸盐(1:2) Chemical Name: 2-[2-[4-[Bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetic acid
CAS No. 150756-35-7, 225367-66-8 (diHCl)
项目整合开发状态: Phase III
项目研究机构: UCB (Originator)
合成路线:The condensation of 1-(4-chlorodiphenylmethyl)piperazine (I) with methyl 2-(2-chloroethoxy)acetate (II) by means of Na2CO3 in refluxing xylene gives methyl 2-[2-[4-(4-chlorodiphenylmethyl)-1-piperazinyl]ethoxy]acetate (III),which is then hydrolyzed with KOH tn reftuxing ethanol.
合成路线:Efletirizine can be obtained by two similar ways:1) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetamide (II) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetamide (III),which is then hydrolyzed with 4N NaOH in refluxing ethanol.2) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetic acid methyl ester (IV) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetic acid methyl ester amide (V),which is then hydrolyzed with 1N KOH in refluxing ethanol.
📌 参考资料/链接：
参考文献标题:Novel 2-[4-(diphenylmethyl)-1-piperazinyl]acetic acids and their amides,process for their preparation and pharmaceutical compsns.Containing them
文献作者:Baltes,E.; De Lannoy,J.; Rodriguez,L.(UCB SA)
参考来源:EP 0058146; US 4525358
📄 详细内容
合成路线:Efletirizine can be obtained by two similar ways:1) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetamide (II) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetamide (III),which is then hydrolyzed with 4N NaOH in refluxing ethanol.2) The condensation of 1-[bis(4-fluorophenyl)methyl]piperazine (I) with 2-(2-chloroethoxy)acetic acid methyl ester (IV) by means of Na2CO3 in hot xylene gives 2-[2-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]ethoxy]acetic acid methyl ester amide (V),which is then hydrolyzed with 1N KOH in refluxing ethanol.
参考文献标题:Efletirizine
文献作者:Graul,A.; Leeson,P.; Castar,R.M.
参考来源:Drugs Fut 1997,22(6),626
产品链接: CAS No. 150756-35-7›› 产品链接: CAS No.225367-66-8››