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【结 构 式】 
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【药物名称】Urapidil, B-66256, Eupressyl, Ebrantil 【化学名称】6-[3-[4-(2-Methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethyluracil 【CA登记号】34661-75-1 【 分 子 式 】C20H29N5O3 【 分 子 量 】387.48583 |
【开发单位】Altana Pharma (Originator), Kaken (Licensee) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, RENAL-UROLOGIC DRUGS, Urologic Drugs, alpha1-Adrenoceptor Antagonists |
合成路线1
Compound can be prepared in two different ways: 1) By condensation of o-methoxyphenylpiperazine carbonate (I) with 1,3-dimethyl-4-(3-chloropropylamino)uracil (II) in refluxing water. 2) By condensation of N-(o-methoxyphenyl)-N'-(3-aminopropyl)piperazine (III) with 1,3-dimethyl-4-chlorouracil (IV) in refluxing triethylamine.
| 【1】 Pruesse, W.; et al.; Aryl-substituted piperazinyl-alkylamino-uracils, -uracil ethers and -uracil thioethers and method for their production. FR 2073300; GB 1309324; US 3957786; US 4067982 . |
| 【2】 Castaner, J.; Garcia-Rafanell, J.; Urapidil. Drugs Fut 1978, 3, 5, 397. |
| 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) | 11882 | 1-(2-Methoxyphenyl)piperazine; Methyl 2-piperazinophenyl ether; 1-(2-Methoxyphenyl)-piperazine | 35386-24-4 | C11H16N2O | 详情 | 详情 |
| (II) | 33441 | 6-[(3-chloropropyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione | C9H14ClN3O2 | 详情 | 详情 | |
| (III) | 33442 | 3-[4-(2-methoxyphenyl)-1-piperazinyl]propylamine; 3-[4-(2-methoxyphenyl)-1-piperazinyl]-1-propanamine | C14H23N3O | 详情 | 详情 | |
| (IV) | 13978 | 6-Chloro-1,3-dimethyluracil; 6-Chloro-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione | 6972-27-6 | C6H7ClN2O2 | 详情 | 详情 |