Bretazenil, Ro-16-6028/000, Ro-16-6028
溴他西尼Chemical Name: (S)-8-Bromo-9-oxo-11,12,13,13a-tetrahydro-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid tert-butyl ester
CAS No. 84379-13-5
项目整合开发状态: Phase III
项目研究机构: Roche (Originator)
合成路线:5-Bromo-2H-3,1-benzoxazine-2,4(1H)-dione (I) and L-proline (II) are heated in DMF to form (S)-6-bromo-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H)-dione (III).This lactam is then reacted with t-BuOK and diphenyl chlorophosphate,and subsequently with the anion of tert-butyl isocyanoacetate.
📌 参考资料/链接：
参考文献标题:Imidazodiazepines,process for their preparation a
文献作者:Hunkeler,W.; Kyburz,E.(F.Hoffmann-La Roche AG)
参考来源:EP 0059391; US 4353827
📄 详细内容
合成路线:5-Bromo-2H-3,1-benzoxazine-2,4(1H)-dione (I) and L-proline (II) are heated in DMF to form (S)-6-bromo-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H)-dione (III).This lactam is then reacted with t-BuOK and diphenyl chlorophosphate,and subsequently with the anion of tert-butyl isocyanoacetate.
参考文献标题:Ro 16-6028
文献作者:Roncari,G.; Jauch,R.; Timm,U.; Pieri,L.; Merz,W.A.; Hunkeler,W.
参考来源:Drugs Fut 1988,13(8),730
产品链接: CAS No. 84379-13-5››