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【结 构 式】 
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【药物名称】GW-505524B 【化学名称】N-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-N-[2-(methylsulfonyl)phenyl]amine 【CA登记号】305809-45-4, 305809-46-5 (fumarate salt), 305809-64-7 (monohydrochloride) 【 分 子 式 】C11H15N3O2S 【 分 子 量 】253.3251 |
【开发单位】GlaxoSmithKline (Originator) 【药理作用】RENAL-UROLOGIC DRUGS, Urinary Incontinence Therapy, alpha1A-Adrenoceptor Agonists |
合成路线1
2-(Methylthio)aniline (I) was alkylated with 2-(chloromethyl)-2-imidazoline hydrochloride (II) in phenol at 120 C to afford the condensation product (III). Subsequent oxidation of the thioether functionality of (III) with m-chloroperbenzoic acid gave rise to the target sulfone.
| 【1】 Hodson, S.J.; Navas, F. III; Bishop, M.J.; Bigham, E.C.; Garrison, D.T.; Drewry, D.H.; Speake, J.D. (Glaxo Group Ltd.); Imidazoline derivs. as alpha-1A adrenoceptor ligands. WO 0066563 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 49148 | 2-(Methylthio)aniline; o-Aminothioanisole; o-Thioanisidine; 2-Aminothioanisole; 2-Methylmercaptoaniline; o-(methylthio)aniline | 2987-53-3 | C7H9NS | 详情 | 详情 |
| (II) | 17330 | 2-(chloromethyl)-4,5-dihydro-1H-imidazole | C4H7ClN2 | 详情 | 详情 | |
| (III) | 49149 | N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-N-[2-(methylsulfanyl)phenyl]amine; N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2-(methylsulfanyl)aniline | C11H15N3S | 详情 | 详情 |
Extended Information