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【结 构 式】 
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【分子编号】24016 【品名】1-methyl-4-phenyl-4-piperidinol 【CA登记号】 |
【 分 子 式 】C12H17NO 【 分 子 量 】191.27312 【元素组成】C 75.35% H 8.96% N 7.32% O 8.36% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(III)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 |
合成路线2
该中间体在本合成路线中的序号：(III)The reaction of N-methyl-4-piperidone (II) with phenyllithium (I) in benzene-ethyl ether below 10 C gives 4-hydroxy-1-methyl-4.phenypiperidine (III), which is dehydrated by treating with refuxing concentrated HCl.
| 【1】 Frank, M.; Clarke, H.Jr. (Novartis Corp.); Nouveaux benzomorphanes et leur preparation. DE 1445845; DE 1795599; FR 1440638; FR 4024M; GB 1050227; US 3320265 . |
| 【2】 Block, F.B.; et al. (Novartis Corp.); Certain 2,6-methano-3-benzazocines. US 3341538 . |
| 【3】 Castaner, J.; Prous, J.; MPTP. Drugs Fut 1986, 11, 5, 384. |
Extended Information