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【结 构 式】 
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【药物名称】Idazoxan hydrochloride, RX-781094 【化学名称】2-[2-(1,4-Benzodioxanyl)]-2-imidazoline hydrochloride 【CA登记号】79944-56-2, 79944-58-4 (free base) 【 分 子 式 】C11H13ClN2O2 【 分 子 量 】240.69146 |
【开发单位】Pierre Fabre (Originator) 【药理作用】Cerebrovascular Diseases, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, beta2-Adrenoceptor Antagonists |
合成路线1
The cyclization of catechol (I) with 2-chloroacrylonitrile (II) by means of K2CO3 in acetone gives 2-cyanobenzo-1,4-dioxane (III), which is hydrolyzed with ethanol and HCl to the corresponding iminoether (IV) Finally, this compound is cyclized with ethylenediamine (V) in cool ethanol.
| 【1】 Myers, P.L.; Chapleo, C.B.; 2-[2-(1,4-Benzodioxanyl)]-2-imidazoline hydrochloride. Tetrahedron Lett 1981, 22, 48, 4839-42. |
| 【2】 Chapleo, C.B.; Myers, P.L. (Reckitt & Colman Pharmaceuticals); Imidazoline deriv.. GB 2068376 . |
| 【3】 Hillier, K.; Idazoxan hydrochloride. Drugs Fut 1983, 8, 9, 778. |
| 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) | 11599 | o-Dihydroxybenzene; Catechol; Pyrocatechol | 120-80-9 | C6H6O2 | 详情 | 详情 |
| (II) | 12372 | 2-Chloroacrylonitrile | 920-37-6 | C3H2ClN | 详情 | 详情 |
| (III) | 36171 | 2,3-dihydro-1,4-benzodioxine-2-carbonitrile | C9H7NO2 | 详情 | 详情 | |
| (IV) | 36172 | ethyl 2,3-dihydro-1,4-benzodioxine-2-carboximidoate | C11H13NO3 | 详情 | 详情 | |
| (V) | 14754 | ethylenediamine;1,2-Diaminoethane;ethane-1,2-diamine；1,2-Ethanediamine | 107-15-3 | C2H8N2 | 详情 | 详情 |
Extended Information