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【结 构 式】 
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【药物名称】Tiapride hydrochloride, Gramalil, Tiapridal 【化学名称】N-[2-(Diethylamino)ethyl]-2-methoxy-5-(methylsulfonyl)benzamide hydrochloride 【CA登记号】51012-33-0, 51012-32-9 (free base) 【 分 子 式 】C15H25ClN2O4S 【 分 子 量 】364.8945 |
【开发单位】Sanofi-synthélabo (Originator), Fujisawa (Licensee) 【药理作用】Antipsychotic Drugs, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS, Tics, Treatment of, Tourette's Syndrome, Treatment of |
合成路线1
Prepared by reacting 2-methoxy-5-methylsulfonylbenzoic acid (I) with isobutyl chloroformate (A) in dioxane to give the corresponding anhydride (II), which is finally condensed with N,N-diethylethylenediamine (B).
| 【1】 Bulteau, G.; Acher, J.; Process for preparing benzamides. CH 585699; DE 2327192; GB 1394563; JP 49085037 . |
| 【2】 Neuman, M.; Prous, J.R.; Tiapride. Drugs Fut 1976, 1, 2, 88. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (B) | 12420 | N-(2-Aminoethyl)-N,N-diethylamine; N,N-Diethylethylene-diamine; N(1),N(1)-Diethyl-1,2-ethanediamine | 100-36-7 | C6H16N2 | 详情 | 详情 |
| (A) | 13423 | 1-[(Chlorocarbonyl)oxy]-2-methylpropane; Isobutyl chloroformate;isobutyl carbonochloridate | 543-27-1 | C5H9ClO2 | 详情 | 详情 |
| (I) | 34068 | 2-methoxy-5-(methylsulfonyl)benzoic acid | 50390-76-6 | C9H10O5S | 详情 | 详情 |
| (II) | 34069 | C14H18O7S | 详情 | 详情 |
Extended Information