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【结 构 式】 
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【药物名称】Naftopidil, KT-611, BM-15275, Avishot, Flivas 【化学名称】(±)-1-[4-(2-Methoxyphenyl)piperazin-1-yl]-3-(1-naphthyloxy)-2-propanol 【CA登记号】57149-07-2 【 分 子 式 】C24H28N2O3 【 分 子 量 】392.50236 |
【开发单位】Roche (Originator), Organon (Not Determined), Asahi Kasei (Licensee) 【药理作用】Benign Prostatic Hyperplasia Therapy, RENAL-UROLOGIC DRUGS, alpha1D-Adrenoceptor Antagonists |
合成路线1
The reaction of 1-naphthol (I) with epichlorohydrin (II) in the presence of aqueous sodium hydroxide yields 1-(1-naphthyloxy)-2,3-epoxypropane (III). (III) is then reacted either in alcohol or without any solvent with 1-(2-methoxyphenyl)piperazine (IV).
| 【1】 Thiel, M.; Sponer, G.; Stach, K.; Witte, E.-C.; Roesch, E. (Roche Diagnostics GmbH); 1-[3-(Napht-1-yloxy)-2-hydroxypropyl]-piperazine c. GB 1445548; US 3997666 . |
| 【2】 Prous, J.; Castaner, J.; Naftopidil. Drugs Fut 1987, 12, 1, 31. |
| 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) | 22935 | alpha-naphthol; 1-naphthol | 90-15-3 | C10H8O | 详情 | 详情 |
| (II) | 10146 | Epichlorohydrin; 2-(Chloromethyl)oxirane | 106-89-8 | C3H5ClO | 详情 | 详情 |
| (III) | 22937 | 2-[(1-naphthyloxy)methyl]oxirane; 1-naphthyl 2-oxiranylmethyl ether | C13H12O2 | 详情 | 详情 | |
| (IV) | 11882 | 1-(2-Methoxyphenyl)piperazine; Methyl 2-piperazinophenyl ether; 1-(2-Methoxyphenyl)-piperazine | 35386-24-4 | C11H16N2O | 详情 | 详情 |
Extended Information