|
【结 构 式】 
|
【药物名称】B-77781 【化学名称】4-(4-Aminophenoxy)-1-methyl-4-phenylpiperidine 【CA登记号】78104-11-7 【 分 子 式 】C18H22N2O 【 分 子 量 】282.38884 |
【开发单位】Altana Pharma (Originator) 【药理作用】Antidepressants, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS |
合成路线1
Reaction of 1-methyl-4-piperidone (I) with phenyllithium (II) gives 1-methyl-4-phenyl-4-piperidinol (III), which is alkylated with (IV) in NaH/DMF to yield (V), followed by reduction with hydrazine/Raney-Ni.
| 【1】 Eistetter, K.; Kley, H.-P.; Menge, H.G.; Schaefer, H. (Byk Gulden Lomberg Chemische Fabrik GmbH); Anti-depressant and analgesic 4-phenoxypiperidines. US 4333942 . |
| 【2】 Menge, H.G.; Eistetter, K.; Schaefer, H.; Kley, H.-P.; B-777-81. Drugs Fut 1983, 8, 5, 387. |
| 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) | 10919 | 1-Methyl-4-piperidone; 1-Methyltetrahydro-4(1H)-pyridinone; N-Methyl-4-piperidone;1-methylpiperidin-4-one | 1445-73-4 | C6H11NO | 详情 | 详情 |
| (II) | 24014 | Phenyllithium | 591-51-5 | C6H5Li | 详情 | 详情 |
| (III) | 24016 | 1-methyl-4-phenyl-4-piperidinol | C12H17NO | 详情 | 详情 | |
| (IV) | 14153 | 4-Fluoronitrobenzene; 1-Fluoro-4-nitrobenzene | 350-46-9 | C6H4FNO2 | 详情 | 详情 |
| (V) | 36052 | 1-methyl-4-phenyl-4-piperidinyl 4-nitrophenyl ether; 1-methyl-4-(4-nitrophenoxy)-4-phenylpiperidine | C18H20N2O3 | 详情 | 详情 |
Extended Information