Itopride hydrochloride, HSR-803, Itax, Ganaton
盐酸伊托必利 伊托必利 Chemical Name: N-[4-[2-(Dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride
CAS No. 122892-31-3, 122898-67-3 (free base)
项目整合开发状态: Launched-1995
项目研究机构: Abbott (Originator), Axcan (Licensee), Fujisawa (Licensee), Sanofi-Aventis (Licensee)
合成路线:The condensation of 4-hydroxybenzaldehyde (I) with 2-(dimethylamino)ethyl chloride (II) by means of K2CO3 in hot isopropyl ether yields 4-[2-(dimethylamino)ethoxy]benzaldehyde (III),which is treated with hydroxylamine hydrochloride in refluxing ethanol to afford the corresponding oxime (IV).The hydrogenation of (IV) with H2 over RaNi in methanolic ammonia yields 4-[2-(dimethylamino)ethoxy]benzylamine (V),which is finally condensed with 3,4-dimethoxybenzoyl chloride (VI) (obtain303ed from the corresponding acid (VII) with SOCl2) in toluene.
📌 参考资料/链接：
参考文献标题:Amide cpds.,process for preparing the same,and compsn.for activating gastric motor function containing the same
文献作者:Itoh,Y.; Kato,H.; Koshinaka,E.; Ogawa,N.; Nishino,H.; Sakaguchi,J.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:AU 8821862; EP 0306827; JP 1989066153; JP 1989079144; JP 1989085960; JP 1989093568; US 4983633
📄 详细内容
合成路线:The condensation of 4-hydroxybenzaldehyde (I) with 2-(dimethylamino)ethyl chloride (II) by means of K2CO3 in hot isopropyl ether yields 4-[2-(dimethylamino)ethoxy]benzaldehyde (III),which is treated with hydroxylamine hydrochloride in refluxing ethanol to afford the corresponding oxime (IV).The hydrogenation of (IV) with H2 over RaNi in methanolic ammonia yields 4-[2-(dimethylamino)ethoxy]benzylamine (V),which is finally condensed with 3,4-dimethoxybenzoyl chloride (VI) (obtain303ed from the corresponding acid (VII) with SOCl2) in toluene.
参考文献标题:Itopride Hydrochloride
文献作者:Castar,J.; Mealy,N.
参考来源:Drugs Fut 1995,20(12),1220
合成路线:The condensation of 4-hydroxybenzaldehyde (I) with 2-(dimethylamino)ethyl chloride (II) by means of K2CO3 in hot isopropyl ether yields 4-[2-(dimethylamino)ethoxy]benzaldehyde (III),which is treated with hydroxylamine hydrochloride in refluxing ethanol to afford the corresponding oxime (IV).The hydrogenation of (IV) with H2 over RaNi in methanolic ammonia yields 4-[2-(dimethylamino)ethoxy]benzylamine (V),which is finally condensed with 3,4-dimethoxybenzoyl chloride (VI) (obtain303ed from the corresponding acid (VII) with SOCl2) in toluene.
参考文献标题:Synthesis,gastrointestinal prokinetic activity and structure-activity relationships of novel N-[[2-(dialkylamino)ethoxy]benzyl]benzamide derivatives
文献作者:Sakaguchi,J.; Nishino,H.; Ogawa,N.; Iwanaga,Y.; Yasuda,S.; Kato,H.; Ito,Y.
参考来源:Chem Pharm Bull 1992,40(1),202-11
产品链接: CAS No. 122892-31-3›› 产品链接: CAS No.122898-67-3››