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项目整合精选>>>Ebastine, RP-64305, LAS-W-090, W-090, Evastel, No-Sedat, Kestine, Bastel, Ebastel
Ebastine, RP-64305, LAS-W-090, W-090, Evastel, No-Sedat, Kestine, Bastel, Ebastel
依巴斯汀Chemical Name: 4'-tert-Butyl-4-[4-(diphenylmethoxy)piperidin-1-yl]butyrophenone; 4-Diphenylmethoxy-1-[3-(4-tert-butylbenzoyl)propyl]piperidine
CAS No. 90729-43-4
项目整合开发状态: Launched-1990
项目研究机构: Almirall Prodesfarma (Originator), Boryung (Licensee), Dainippon Pharmaceutical (Licensee), High Noon Labs. (Licensee), Meiji Seika (Licensee), Nycomed Pharma (Licensee)
合成路线:This compound can be obtained by two related routes:1) Condensation of 4-hydroxypiperidine (I) with p-tert-butyl-omega-chlorobutyrophenone (II) in hot methyl isobutyl ketone in presence of sodium bicarbonate gives 1-[3-(4-tert-butylbenzoyl)propyl]-4-hydroxypiperidine (III),which reacts with diphenylmethyl bromide (IV) in methyl isobutyl ketone to give ebastine.2) 4-Diphenylmethoxypiperidine (VI),obtained by alkaline hydrolysis of 1-ethoxycarbonyl-4-diphenyl-methoxypiperidine (V) was reacted with p-tert-butyl-omega-chlorobutyrophenone (II) to give ebastine.
📌 参考资料/链接：
参考文献标题:EBASTINE
文献作者:Moragues,J.; Roberts,D.J.
参考来源:Drugs Fut 1990,15(7),674
📄 详细内容
合成路线:This compound can be obtained by two related routes:1) Condensation of 4-hydroxypiperidine (I) with p-tert-butyl-omega-chlorobutyrophenone (II) in hot methyl isobutyl ketone in presence of sodium bicarbonate gives 1-[3-(4-tert-butylbenzoyl)propyl]-4-hydroxypiperidine (III),which reacts with diphenylmethyl bromide (IV) in methyl isobutyl ketone to give ebastine.2) 4-Diphenylmethoxypiperidine (VI),obtained by alkaline hydrolysis of 1-ethoxycarbonyl-4-diphenyl-methoxypiperidine (V) was reacted with p-tert-butyl-omega-chlorobutyrophenone (II) to give ebastine.
参考文献标题:Piperidine derivs
文献作者:Spickett,R.G.W.; Moragues,J.; Prieto,J.; Vega,A.(Fordonal S.A.)
参考来源:EP 0134124B; US 4550116
产品链接: CAS No. 90729-43-4››