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项目整合精选>>>Tiropramide, CR-605, Tirospan, Maioral, Alfospas(HCl), Maiorad(HCl)
Tiropramide, CR-605, Tirospan, Maioral, Alfospas(HCl), Maiorad(HCl)
替瑞酰胺 盐酸替瑞酰胺 Chemical Name: D,L-alpha-Benzamido-p-[2-(diethylamino)ethoxy]-N,N-dipropylhydrocinnamamide; (?-alpha-(Benzoylamino)-4-[2-(diethylamino)ethoxy]-N,N-dipropylbenzenepropanamide
CAS No. 55837-29-1, 57227-16-4 (HCl)
项目整合开发状态: Launched-1983
项目研究机构: Rotta (Originator), Kissei (Licensee)
合成路线:The benzoylation of tyrosine (I) with benzoyl chloride (II) in aqueous NaOH gives O,N-(di-benzoyl)-D,L-tyrosine (III),which by reaction with di-n-propylamine (A) by means of ethyl chlorocarbonate and triethylamine in acetone is converted into O,N-(di-benzoyl)-D,L-tyrosyl-di-n-propylamide (IV).Selective hydrolysis of (IV) with NaOH in methanol - water affords N-benzoyl-D,L-tyrosyl-di-n-propylamide (V),which is finally condensed with 2-(diethylamino)ethyl chloride (VI) by means of sodium methoxide in refluxing toluene.
📌 参考资料/链接：
参考文献标题:O-Tertiary amino-alkyl-N-benzoyl tyrosil amides
文献作者:Makovec,F.; Rovati,L.; Senini,P.(Rotta Research Laboratorium SpA)
参考来源:DE 2503992; FR 2259592; GB 1467927; JP 50116442; NL 167683C; US 4004008
📄 详细内容
合成路线:The benzoylation of tyrosine (I) with benzoyl chloride (II) in aqueous NaOH gives O,N-(di-benzoyl)-D,L-tyrosine (III),which by reaction with di-n-propylamine (A) by means of ethyl chlorocarbonate and triethylamine in acetone is converted into O,N-(di-benzoyl)-D,L-tyrosyl-di-n-propylamide (IV).Selective hydrolysis of (IV) with NaOH in methanol - water affords N-benzoyl-D,L-tyrosyl-di-n-propylamide (V),which is finally condensed with 2-(diethylamino)ethyl chloride (VI) by means of sodium methoxide in refluxing toluene.
参考文献标题:Tiropramide
文献作者:Serradell,M.N.; de Angelis,L.; Blancafort,P.; Castar,J.
参考来源:Drugs Fut 1982,7(6),413
合成路线:The benzoylation of tyrosine (I) with benzoyl chloride (II) in aqueous NaOH gives O,N-(di-benzoyl)-D,L-tyrosine (III),which by reaction with di-n-propylamine (A) by means of ethyl chlorocarbonate and triethylamine in acetone is converted into O,N-(di-benzoyl)-D,L-tyrosyl-di-n-propylamide (IV).Selective hydrolysis of (IV) with NaOH in methanol - water affords N-benzoyl-D,L-tyrosyl-di-n-propylamide (V),which is finally condensed with 2-(diethylamino)ethyl chloride (VI) by means of sodium methoxide in refluxing toluene.
参考文献标题:Activity of derivatives of tyrosine on gastrointestinal motility
文献作者:Senin; et al.
参考来源:Gastrointestinal Motility in Health and Disease.Duthie,H.L.(Ed.); MTP Press Limited,Lancaster 1978,417-427
产品链接: CAS No. 55837-29-1›› 产品链接: CAS No.57227-16-4››