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【结 构 式】 
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【药物名称】 【化学名称】8-[4-[N-(7-Hydroxy-2,3-dihydro-1-benzofuran-2-ylmethyl)-N-propylaminobutyl]-8-azaspiro[4.5]decane-7,9-dione oxalate 【CA登记号】 【 分 子 式 】C27H38N2O8 【 分 子 量 】518.61251 |
【开发单位】Servier (Originator) 【药理作用】Pharmacological Tools, Drugs Acting on 5-Hydroxytryptamine Receptors |
合成路线1
The condensation of 8-methoxy-3,4-dihydro-2H-1-benzopyran-3-amine (I) with 8-(4-bromobutyl)-8-azaspiro[4.5]decane-7,9-dione (II) by means of KI and triethylamine in ot DMF gives the secondary amine (III), which is alkylated with propyliodide and K2CO3 in hot DMF affording the tertiary amine (IV). Finally, this compound is treated with BBr3 in refluxing dichloromethane.
| 【1】 Viaud, M.-C.; Pfeiffer, B.; Guillaumet, G.; Renard, P.; Rettori, M.-C.; Boyé, S.; N,N-Disubstituted aminomethyl benzofuran derivatives: Synthesis and preliminary binding evaluation. Bioorg Med Chem 1999, 7, 2, 335. |
| 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) | 29454 | 8-methoxy-3,4-dihydro-2H-chromen-3-ylamine; 8-methoxy-3-chromanamine | 112904-73-1 | C10H13NO2 | 详情 | 详情 |
| (II) | 29455 | 8-(4-bromobutyl)-8-azaspiro[4.5]decane-7,9-dione | C13H20BrNO2 | 详情 | 详情 | |
| (III) | 29456 | 8-[4-[(8-methoxy-3,4-dihydro-2H-chromen-3-yl)amino]butyl]-8-azaspiro[4.5]decane-7,9-dione | C23H32N2O4 | 详情 | 详情 | |
| (IV) | 29457 | 8-[4-[(8-methoxy-3,4-dihydro-2H-chromen-3-yl)(propyl)amino]butyl]-8-azaspiro[4.5]decane-7,9-dione | C26H38N2O4 | 详情 | 详情 |
Extended Information