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【结 构 式】 
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【药物名称】 【化学名称】Acetic acid 1-[2-(1H-imidazol-4-yl)-1(R)-methylethylcarbamoyloxy]ethyl ester 【CA登记号】 【 分 子 式 】C11H17N3O4 【 分 子 量 】255.27584 |
【开发单位】Freie Universität Berlin (Originator), INSERM (Originator) 【药理作用】Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, PHARMACOLOGICAL TOOLS, Histamine H3 Receptor Agonists |
合成路线1
Treatment of p-nitrophenol (I) with 1-chloroethyl chloroformate (II) in the presence of pyridine afforded carbonate (III). Subsequent displacement of the chlorine atom of (III) with mercuric acetate in HOAc provided the acetoxy derivative (IV). This was then condensed with (R)-alpha-methylhistamine (V) in HMPT to furnish the title compound.
| 【1】 Stark, H.; et al.; Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist (R)-alpha-methylhistamine. Bioorg Med Chem 2001, 9, 1, 191. |
| 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) | 11236 | 4-Nitrophenol; p-Nitrophenol | 100-02-7 | C6H5NO3 | 详情 | 详情 |
| (II) | 22014 | 1-chloro-1-[(chlorocarbonyl)oxy]ethane | 50893-53-3 | C3H4Cl2O2 | 详情 | 详情 |
| (III) | 51393 | 1-chloroethyl 4-nitrophenyl carbonate | C9H8ClNO5 | 详情 | 详情 | |
| (IV) | 50378 | 1-[[(4-nitrophenoxy)carbonyl]oxy]ethyl acetate | C11H11NO7 | 详情 | 详情 | |
| (V) | 51394 | (2R)-1-(1H-imidazol-4-yl)-2-propanamine; (1R)-2-(1H-imidazol-4-yl)-1-methylethylamine | C6H11N3 | 详情 | 详情 |
Extended Information