【药物名称】Apraclonidine hydrochloride, p-Aminoclonidine hydrochloride, Aplonidine hydrochloride, ALO-2145, Iopidine
化学结构式(Chemical Structure):
参考文献No.9842
标题:Method for lowering intraocular pressure using phenylimino-imidazoles
作者:York, B.M. Jr. (Alcon Laboratories, Inc.)
来源:US 4517199
合成路线图解说明:

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No.48431
标题:Method of lowering intraocular pressure using phenylimino-imidazoles
作者:Cavero, I.; Langer, S.Z.; York, B.M. Jr.
来源:US 4515800
合成路线图解说明:

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No.63005
标题:Aplonidine hydrochloride
作者:Prous, J.; Casta馿r, J.
来源:Drugs Fut 1988,13(6),507
合成路线图解说明:

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.

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