|
【结 构 式】 
|
【药物名称】Triazolam, U-33030, Hypnostat, Halcion 【化学名称】8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-1,2,4-triazolo[4,3-a][1,4]benzodiazepine 【CA登记号】28911-01-5 【 分 子 式 】C17H12Cl2N4 【 分 子 量 】343.21799 |
【开发单位】Pfizer (Originator), Questcor (Not Determined), Fabre-Kramer (Licensee) 【药理作用】PSYCHOPHARMACOLOGIC DRUGS, Sedative/Hypnotics, Sleep Disorders, Treatment of, Benzodiazepines, GABA(A) BZ Site Receptor Agonists |
合成路线1
By cyclization of 2-glycylamino-2',5-dichlorobenzenophenone (I) in pyridine to give 7-chloro-5-(o-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one (II), which was refluxed with P2S5 in pyridine yielding 7-chloro-5-(o-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-thione (III). Finally, this product was condensed with acetylhydrazide (A) in butanol.
| 【1】 Sternbach, L.H.; 1,4-Benzodiazepines. Chemistry and some aspects of the structure activity relationship. Angew Chem 1971, 10, 34-43. |
| 【2】 Hester, J.B. Jr.; 6-Phenyl-4H-S-triazolo[4,3-a][1,4]benzodiazepines. DE 2012190; FR 2034999; GB 1291631; US 3987052 . |
| 【3】 Castaner, J.; Chatterjee, S.S.; Triazolam. Drugs Fut 1976, 1, 8, 393. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (A) | 29262 | acetohydrazide | 1068-57-1 | C2H6N2O | 详情 | 详情 |
| (I) | 34116 | 2-amino-N-[4-chloro-2-(2-chlorobenzoyl)phenyl]acetamide | C15H12Cl2N2O2 | 详情 | 详情 | |
| (II) | 34117 | 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one | C15H10Cl2N2O | 详情 | 详情 | |
| (III) | 34118 | 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepine-2-thione | C15H10Cl2N2S | 详情 | 详情 |