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Apraclonidine hydrochloride, p-Aminoclonidine hydrochloride, Aplonidine hydrochloride, ALO-2145, Iopidine

盐酸安普乐定Chemical Name: 2-(4-Amino-2,6-dichloro)phenyliminoimidazolidine hydrochloride
CAS No. 73218-79-8
项目整合开发状态: Launched-1988
项目研究机构: Alcon (Originator)
合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.
📌 参考资料/链接:
参考文献标题:Method for lowering intraocular pressure using phenylimino-imidazoles
文献作者:York,B.M.Jr.(Alcon Laboratories,Inc.)
参考来源:US 4517199

📄 详细内容


合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.

参考文献标题:Method of lowering intraocular pressure using phenylimino-imidazoles
文献作者:Cavero,I.; Langer,S.Z.; York,B.M.Jr.
参考来源:US 4515800


合成路线:The cyclization of 2-amino-4'-bromobenzophenone (I) with ethyl 2-(methylthio)acetate (II) by means of tert-butyl hypochlorite in dichloromethane at 70 C gives 7-(4-bromobenzoyl)-3-(methylthio)-2,3-dihydro-1H-indol-2-one (III),which is desulfurized by a treatment with Raney Nickel in THF yielding 7-(4-bromobenzoyl)-2,3-dihydro-1H-indol-2-one (IV).Finally,this compound is hydrolyzed with refluxing 3N NaOH and acidified with concentrated HCl.
参考文献标题:Aplonidine hydrochloride
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(6),507


产品链接: CAS No. 73218-79-8››