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【结 构 式】 
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【药物名称】KT-362 【化学名称】5-[N-[2-(3,4-Dimethoxyphenyl)ethyl]-beta-alanyl]-2,3,4,5-tetrahydrobenzo-1,5-thiazepine bifumarate 【CA登记号】105394-80-7 【 分 子 式 】C26H32N2O7S 【 分 子 量 】516.61814 |
【开发单位】Kotobuki (Originator) 【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Calcium Channel Blockers |
合成路线1
The acylation of 2,3,4,5-tetrahydrobenzo-1,5 thiazepine (I) with 3-bromopropionyl bromide (II) by means of pyridine in toluene gives 5-(3-bromo-propionyl)-2,3,4,5 tetrahydrobenzo-1,5-thiazepine (III), which is then condensed with 2-(3,4-dimethoxyphenyl)ethylamine (IV) in refluxing dichloromethane, and treated with fumaric acid.
| 【1】 Tomiyama, T. (Kotobuki Pharmaceutical Co., Ltd.); Antihypertensive 1,5-benzothiazepine derivs. and compsns. thereof. US 4584292 . |
| 【2】 Prous, J.; Castaner, J.; KT-362. Drugs Fut 1988, 13, 7, 622. |
| 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) | 22617 | 2,3,4,5-tetrahydro-1,5-benzothiazepine | C9H11NS | 详情 | 详情 | |
| (II) | 22618 | 3-bromopropanoyl bromide | C3H4Br2O | 详情 | 详情 | |
| (III) | 22619 | 3-bromo-1-[3,4-dihydro-1,5-benzothiazepin-5(2H)-yl]-1-propanone | C12H14BrNOS | 详情 | 详情 | |
| (IV) | 10098 | 2-(3,4-Dimethoxyphenyl)-1-ethanamine; 3,4-Dimethoxyphenethylamine; 2-(3,4-Dimethoxyphenyl)ethylamine | 120-20-7 | C10H15NO2 | 详情 | 详情 |
Extended Information