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【结 构 式】 
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【药物名称】Ro-11-1464 【化学名称】9-Methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine 【CA登记号】54123-09-0 【 分 子 式 】C15H12N4S 【 分 子 量 】280.35369 |
【开发单位】Roche (Originator) 【药理作用】Angina pectoris, Treatment of, CARDIOVASCULAR DRUGS, Treatment of Disorders of the Coronary Arteries and Atherosclerosis |
合成路线1
Treatment of diazepinone (I) with phosphorus pentasulfide in refluxing pyridine affords diazepinethione (II). Subsequent reaction with acetyl hydrazine in refluxing n-butanol gives the intermediate acetylhydrazino compound (III), which on prolonged heating cyclizes to the desired triazolodiazepine.
| 【1】 Hellerbach, J.; Zeller, P.; Binder, D.; Hromatka, O. (F. Hoffmann-La Roche AG); Diazepine derivs.. DE 2405682; GB 1456161; US 4155913 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 29262 | acetohydrazide | 1068-57-1 | C2H6N2O | 详情 | 详情 | |
| (I) | 19204 | 5-phenyl-1,3-dihydro-2H-thieno[2,3-e][1,4]diazepin-2-one | C13H10N2OS | 详情 | 详情 | |
| (II) | 19205 | 5-phenyl-1,3-dihydro-2H-thieno[2,3-e][1,4]diazepine-2-thione | C13H10N2S2 | 详情 | 详情 | |
| (III) | 19206 | N'-(5-phenyl-3H-thieno[2,3-e][1,4]diazepin-2-yl)acetohydrazide | C15H14N4OS | 详情 | 详情 |
Extended Information