|
【结 构 式】 
|
【药物名称】Bunazosin hydrochloride, E-1015(retard), E-643, Andante, Detantol 【化学名称】4-Amino-6,7-dimethoxy-2-[4-(n-butyryl)homopiperazin-1-yl]quinazoline hydrochloride 【CA登记号】52712-76-2, 80755-51-7 (free base) 【 分 子 式 】C19H28ClN5O3 【 分 子 量 】409.91971 |
【开发单位】Eisai (Originator), Boehringer Ingelheim (Licensee), Santen (Licensee) 【药理作用】Antiglaucoma Agents, CARDIOVASCULAR DRUGS, Hypertension, Treatment of, OCULAR MEDICATIONS, Ophthalmic Drugs, alpha1-Adrenoceptor Antagonists |
合成路线1
Compound can be prepared in two different ways: 1) By condensation of 2-chloro-4-amino-5,7-dimethoxyquinazoline (I) with 1-(n-butyryl)homopiperazine (II) in refluxing butanol. 2) By cyclization of 2-amino-4,5-dimethoxybenzonitrile (III) with 4-(n-butyryl)homopiperazin-1-formamidine (IV), by means of sodium methoxide in refluxing dimethylsulfoxide.
| 【1】 Takahashi, T.; Sugimoto, H.; JP 75140474 . |
| 【2】 Takahashi, T.; Sugimoto, H.; JP 7682285 . |
| 【3】 Castaner, J.; Weetman, D.F.; E-643. Drugs Fut 1978, 3, 8, 582. |
| 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) | 10443 | 2-Chloro-6,7-dimethoxy-4-quinazolinamine; 4-Amino-2-chloro-6,7-dimethoxyquinazoline; 2-Chloro-6,7-dimethoxy-4-quinazolinylamine | 23680-84-4 | C10H10ClN3O2 | 详情 | 详情 |
| (II) | 33529 | 1-(1,4-diazepan-1-yl)-1-butanone | 61903-12-6 | C9H18N2O | 详情 | 详情 |
| (III) | 13038 | 2-Amino-4,5-dimethoxybenzonitrile | 26961-27-3 | C9H10N2O2 | 详情 | 详情 |
| (IV) | 33530 | 4-butyryl-1,4-diazepane-1-carboximidamide; 1-amidino-4-butyrylhomopiperazine | 59775-30-3 | C10H20N4O | 详情 | 详情 |