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【结 构 式】 
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【药物名称】Premazepam, MDL-181, DL-181 【化学名称】3,7-Dihydro-6,7-dimethyl-5-phenylpyrrolo[3,4-d]-1,4-diazepin-2(1H)-one 【CA登记号】57435-86-6 【 分 子 式 】C15H15N3O 【 分 子 量 】253.3063 |
【开发单位】Lepetit (Originator) 【药理作用】Anxiolytics, PSYCHOPHARMACOLOGIC DRUGS, Benzodiazepines, GABA(A) BZ Site Receptor Agonists |
合成路线1
The reaction of 1,2-dimethyl-3-benzoyl-4-aminopyrrole (I) with phthalimidoacetyl chloride (II) by means of NaOH gives 1,2-dimethyl-3-benzoyl-4-(phthalimidoacetamido)pyrrole (III), which is cyclized by reaction with hydrazine in refluxing methanol.
| 【1】 Corsico, N.; Tarzia, G.; Fontanella, L.; Mariani, L.; 3,7-Dihydro-5-phenylpyrrolo[3,4-e][1,4]diazepin-2(1H)-ones. Synthesis and pharmaclogical properties. Eur J Med Chem - Chim Ther 1976, 11, 3, 217-220. |
| 【2】 Fontanella, L.; Mariani, L.; Tarzia, G.; Pharmacologically active pyrrolodiazepines. DE 2511599; FR 2264546; GB 1433103; JP 50135094; US 4022766; US 4022766 . |
| 【3】 Castaner, J.; Serradell, M.N.; Premazepam. Drugs Fut 1984, 9, 7, 520. |
| 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) | 34365 | N'-(2-ethylbenzoyl)-3-methoxybenzenecarbohydrazonamide | C17H19N3O2 | 详情 | 详情 | |
| (II) | 10278 | 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)acetyl chloride | 6780-38-7 | C10H6ClNO3 | 详情 | 详情 |
| (III) | 34367 | N-(4-benzoyl-1,5-dimethyl-1H-pyrrol-3-yl)-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)acetamide | C23H19N3O4 | 详情 | 详情 |
Extended Information