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【结 构 式】 
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【药物名称】Remoxipride, FLA-731, A-33547, Roxiam 【化学名称】(-)-(S)-3-Bromo-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2,6-dimethoxybenzamide 【CA登记号】80125-14-0, 82935-42-0 (HCl) 【 分 子 式 】C16H23BrN2O3 【 分 子 量 】371.27731 |
【开发单位】AstraZeneca (Originator), Bracco (Licensee) 【药理作用】Antipsychotic Drugs, PSYCHOPHARMACOLOGIC DRUGS, Dopamine D2 Antagonists |
合成路线1
The bromination of 2,6-dimethoxybenzoic acid (I) with Br2 in dioxane gives 3-bromo-2,6-dimethoxy benzoic acid (II), which is treated with refluxing SOCl2 yielding the corresponding acyl chloride (III). Finally, this compound is condensed with (-)-(S)-1-ethyl 2-(aminomethyl)pyrrolidine (IV).
| 【1】 Florvall, L.; Ogren, S.O.; Potential neuroleptic agents. 2,6-dialkoxybenzamide derivatives with potent dopamine receptor blocking activities. J Med Chem 1982, 25, 11, 1280. |
| 【2】 Prous, J.; Castaner, J.; Remoxipride. Drugs Fut 1986, 11, 11, 944. |
| 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) | 24193 | 2,6-dimethoxybenzoic acid | 1466-76-8 | C9H10O4 | 详情 | 详情 |
| (II) | 24194 | 3-bromo-2,6-dimethoxybenzoic acid | 73219-89-3 | C9H9BrO4 | 详情 | 详情 |
| (III) | 24195 | 3-bromo-2,6-dimethoxybenzoyl chloride | C9H8BrClO3 | 详情 | 详情 | |
| (IV) | 21345 | (2S)-1-Ethyl-2-(aminomethyl)pyrrolidine; [(2S)-1-Ethylpyrrolidinyl]methanamine | C7H16N2 | 详情 | 详情 |
Extended Information