LY-127210
7,8-二甲氧基-1H-3-苯并氮杂卓-2-胺盐酸盐Chemical Name: 7,8-Dimethoxy-1H-3-benzazepine-2-amine hydrochloride
CAS No. 93270-40-7
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:The condensation of 3,4-dimethoxyphenyacetic acid (I) with 2-aminoacetaldehyde diethylacetal (II) by means of 1,1'-carbonyldiimidazole (CDI) in CHCl3 gives N-(2,2-diethoxyethyl)-3,4-dimelhoxyphenylacetamide (III),which is cyclized by means of 48% aqueous HBr yielding 1,3-dihydro-7,8-dimethoxy-2H-3-benzazepin-2-one (IV).The reaction of (IV) with triethyloxonium tetrafluoroborate (V) in methylene chloride affords 2-ethoxy-7,8-dimethoxy-1H-3-benzazepine (VI),which is finally treated with ammonium chloride in refluxing methanol.
📌 参考资料/链接：
参考文献标题:Benzazepine derivs.
文献作者:Paget,C.J.Jr.; Ruffolo,R.R.Jr.(Eli Lilly and Company)
参考来源:EP 0116444; ES 8602681; ES 8801215; GB 2134519
📄 详细内容
合成路线:The condensation of 3,4-dimethoxyphenyacetic acid (I) with 2-aminoacetaldehyde diethylacetal (II) by means of 1,1'-carbonyldiimidazole (CDI) in CHCl3 gives N-(2,2-diethoxyethyl)-3,4-dimelhoxyphenylacetamide (III),which is cyclized by means of 48% aqueous HBr yielding 1,3-dihydro-7,8-dimethoxy-2H-3-benzazepin-2-one (IV).The reaction of (IV) with triethyloxonium tetrafluoroborate (V) in methylene chloride affords 2-ethoxy-7,8-dimethoxy-1H-3-benzazepine (VI),which is finally treated with ammonium chloride in refluxing methanol.
参考文献标题:LY-127210
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1986,11(9),748
产品链接: CAS No. 93270-40-7››