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【结 构 式】 
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【药物名称】Diprafenone 【化学名称】(±)-2'-[2-Hydroxy-3-(tert-pentylamino)propoxy]-3-phenylpropiophenone 【CA登记号】81447-80-5, 86342-43-0 (HCl) 【 分 子 式 】C23H31NO3 【 分 子 量 】369.50842 |
【开发单位】Helopharm (Originator) 【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS, beta-Adrenoceptor Antagonists |
合成路线1
The condensation of 2'-hydroxy-3-phenylpropiophenone (I) with 1 chloro-2,3-epoxypropane (II) by means of K2CO3 gives 2'-(2,3-epoxypropoxy)-3-phenylpropiophenone (III), which is then treated with 2-methyl-2-aminobutane (IV) in refluxing methanol.
| 【1】 Petrik, G.; Sachse, R. (Helopharm KG); 2-[2'-Hydroxy-3'-(1,1-dimethylpropylamino)-propoxy]-beta-phenylpropiophenone, its physiologically acceptable acid addition salts, and pharmaceutical compsns.. DE 3133814; US 4460605 . |
| 【2】 Prous, J.; Castaner, J.; Difrafenone. Drugs Fut 1986, 11, 8, 645. |
| 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) | 24436 | 1-(2-hydroxyphenyl)-3-phenyl-1-propanone | 42772-82-7 | C15H14O2 | 详情 | 详情 |
| (II) | 10146 | Epichlorohydrin; 2-(Chloromethyl)oxirane | 106-89-8 | C3H5ClO | 详情 | 详情 |
| (III) | 24438 | 1-[2-(2-oxiranylmethoxy)phenyl]-3-phenyl-1-propanone | C18H18O3 | 详情 | 详情 | |
| (IV) | 24439 | 2-methyl-2-butanamine | 594-39-8 | C5H13N | 详情 | 详情 |
Extended Information