Timelotem maleate, KC-7507
替美洛坦 Chemical Name: (?-10-Fluoro-1,2,3,4,4a,5-hexahydro-3-methyl-7-(2-thienyl)pyrazino[1,2-a][1,4]benzodiazepine dihydrogenmaleate
CAS No. 105138-32-7, 96306-34-2 (free base)
项目整合开发状态: Preclinical
项目研究机构: Kali-Chemie (Originator)
合成路线:Timelotem can be prepared by cyclization of the acyl diamine (I) with phosphorus oxychloride at 80-130 C,yielding the ring isomers (II) and (III).At higher reaction temperatures (II) is formed almost exclusively.It can be separated into its enantiomers.Subsequent reaction with methylamine -either of the crude mixture of (II) and (III) or of the pure racemic or enantiomeric (II)- affords anellation te yield title compound.
📌 参考资料/链接：
参考文献标题:[1,2]-Fused 1,4-benzodiazepine cpds.,process for
文献作者:Benson,W.; Heinemann,H.; Liepmann,H.; Muesch,H.; Ruhland,M.; Zeugner,H.(Kali-Chemie AG)
参考来源:DE 3151597; EP 0084155; US 4508716
📄 详细内容
合成路线:Timelotem can be prepared by cyclization of the acyl diamine (I) with phosphorus oxychloride at 80-130 C,yielding the ring isomers (II) and (III).At higher reaction temperatures (II) is formed almost exclusively.It can be separated into its enantiomers.Subsequent reaction with methylamine -either of the crude mixture of (II) and (III) or of the pure racemic or enantiomeric (II)- affords anellation te yield title compound.
参考文献标题:7-Phenyl-1,4-benzodiazepine derivs.
文献作者:Hell,I.; Hueschens,R.; Liepmann,H.; Milkowski,W.; Wolf,K.-U.; Zeugner,H.(Kali-Chemie AG)
参考来源:EP 0008045; US 4338314
合成路线:Timelotem can be prepared by cyclization of the acyl diamine (I) with phosphorus oxychloride at 80-130 C,yielding the ring isomers (II) and (III).At higher reaction temperatures (II) is formed almost exclusively.It can be separated into its enantiomers.Subsequent reaction with methylamine -either of the crude mixture of (II) and (III) or of the pure racemic or enantiomeric (II)- affords anellation te yield title compound.
参考文献标题:Timelotem maleate
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(5),424
产品链接: CAS No.96306-34-2››