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【结 构 式】 
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【药物名称】 【化学名称】N-[2-[N-(5-Methoxy-1,2,3,4-tetrahydronaphth-2-yl)-N-propylamino]ethyl]benzamide hydrochloride 【CA登记号】220772-95-2, 220772-98-5 (HCl) 【 分 子 式 】C23H31ClN2O2 【 分 子 量 】402.96872 |
【开发单位】AstraZeneca (Originator) 【药理作用】Antipsychotic Drugs, PSYCHOPHARMACOLOGIC DRUGS, 5-HT1A Receptor Agonists, Dopamine D2 Antagonists |
合成路线1
Alkylation of aminotetralin (I) with bromoacetonitrile in boiling acetone gave cyanomethyl compound (II). This was subsequently reduced to diamine (III) using LiAlH4. Condensation of (III) with benzoyl chloride under Schotten-Baumann conditions then yielded the corresponding benzamide.
| 【1】 Homan, E.J.; Copinga, S.; Elfström, L.; van der Veen, T.; Hallema, J.-P.; Mohell, N.; Unelius, L.; Johansson, R.; Wikström, H.V.; Grol, C.J.; 2-Aminotetralin-derived substituted benzamides with mixed dopamine D2, D3, and serotonin 5-HT1A receptor binding properties: A novel class of potential atypical antipsychotic agents. Bioorg Med Chem 1998, 6, 11, 2111. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 10463 | Benzoyl chloride | 98-88-4 | C7H5ClO | 详情 | 详情 | |
| 31883 | 2-bromoacetonitrile | 590-17-0 | C2H2BrN | 详情 | 详情 | |
| (I) | 14648 | N-(5-methoxy-1,2,3,4-tetrahydro-2-naphthalenyl)-N-propylamine; 5-methoxy-N-propyl-1,2,3,4-tetrahydro-2-naphthalenamine | C14H21NO | 详情 | 详情 | |
| (II) | 27938 | 2-[(5-methoxy-1,2,3,4-tetrahydro-2-naphthalenyl)(propyl)amino]acetonitrile | C16H22N2O | 详情 | 详情 | |
| (III) | 27939 | N-(2-aminoethyl)-N-(5-methoxy-1,2,3,4-tetrahydro-2-naphthalenyl)-N-propylamine | C16H26N2O | 详情 | 详情 |
Extended Information