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项目整合精选>>>Nizatidine, ZE-101, ZL-101, LY-139037, Zanizal, Nizax, Acinon, Axid
Nizatidine, ZE-101, ZL-101, LY-139037, Zanizal, Nizax, Acinon, Axid
尼扎替丁Chemical Name: N-[2-[2-[(Dimethylamino)methyl]-4-thiazolylmethylthio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine
CAS No. 76963-41-2
项目整合开发状态: Launched-1987
项目研究机构: Lilly (Originator), Italfarmaco (Licensee), Reliant Pharmaceuticals (Licensee), Zeria (Licensee)
合成路线:The cyclization of dimethylaminothioacetamide (I) with ethyl bromopyruvate (II) in refluxing ethanol gives ethyl 2-(dimethylaminomethyl)-4-thiazolecarboxylate (III),which is reduced with lithium triethyl borohydride in THF yielding 2-(dimethylaminomethyl)-4-thiazolemethanol (IV).The condensation of (IV) with 2-aminoethanethiol (V) by means of 48% HBr affords 2-(dimethylaminomethyl)-4-(2-aminoethylthiomethyl)thiazole (VI),which is finally condensed with 1-(methylthio)-2-nitro-N-methylethyleneamine (VII) in water.
📌 参考资料/链接：
参考文献标题:N-Methyl-N'-2-[[(2-dimethylaminomethyl)-4-thiazolyl]methylthio]ethyl-2-nitro-1,1-ethenediamine
文献作者:Pioch,R.P.(Eli Lilly and Company)
参考来源:EP 0049618; GB 2084581; JP 57091980; US 4375547
📄 详细内容
合成路线:The cyclization of dimethylaminothioacetamide (I) with ethyl bromopyruvate (II) in refluxing ethanol gives ethyl 2-(dimethylaminomethyl)-4-thiazolecarboxylate (III),which is reduced with lithium triethyl borohydride in THF yielding 2-(dimethylaminomethyl)-4-thiazolemethanol (IV).The condensation of (IV) with 2-aminoethanethiol (V) by means of 48% HBr affords 2-(dimethylaminomethyl)-4-(2-aminoethylthiomethyl)thiazole (VI),which is finally condensed with 1-(methylthio)-2-nitro-N-methylethyleneamine (VII) in water.
参考文献标题:Nizatidine
文献作者:Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1984,9(9),655
产品链接: CAS No. 76963-41-2››