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【结 构 式】 
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【药物名称】Tilisolol hydrochloride, N-696, Daim, Selecal 【化学名称】(±)-4-[3-(tert-Butylamino)-2-hydroxypropoxy]-N-methylisocarbostyril monohydrochloride 【CA登记号】85136-71-6 (free base), 62774-96-3 (undefined isomer) 【 分 子 式 】C17H25ClN2O3 【 分 子 量 】340.8534 |
【开发单位】Nisshin Pharma (Originator), Toyama (Originator) 【药理作用】Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, beta-Adrenoceptor Antagonists |
合成路线1
The condensation of N-methyl-4-hydroxyisocarbostyril (I) with epichlorohydrin (II) by means of sodium methoxide in hot methanol gives 4-(2,3-epoxypropoxy)-N-methylisocarbostyril (III), which is then treated with tert-butylamine (IV) in methanol, and with HCl.
| 【1】 Fukushima, H.; Suzuki, Y. (Nisshin Flour Milling Co., Ltd.); Isocarbostyril derivatives. DE 2631080; GB 1501149; JP 52012178 . |
| 【2】 Serradell, M.N.; Blancafort, P.; Thorpe, P.J.; Castaner, J.; N-696. Drugs Fut 1982, 7, 12, 889. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 17895 | 2-Amino-2-methylpropane; tert-butylamine; 2-methyl-2-propanamine | 75-64-9 | C4H11N | 详情 | 详情 | |
| (I) | 32094 | 4-hydroxy-2-methyl-1(2H)-isoquinolinone | C10H9NO2 | 详情 | 详情 | |
| (II) | 10146 | Epichlorohydrin; 2-(Chloromethyl)oxirane | 106-89-8 | C3H5ClO | 详情 | 详情 |
| (III) | 32095 | 2-methyl-4-(2-oxiranylmethoxy)-1(2H)-isoquinolinone | C13H13NO3 | 详情 | 详情 |