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项目整合精选>>>Metuclazepam, Brometazepam, Metaclazepam, KC-2547, KA-2547, Talis
Metuclazepam, Brometazepam, Metaclazepam, KC-2547, KA-2547, Talis
甲酯 7-溴-5-(2-氯苯基)-2,3-二氢-2-(甲氧基甲基)-1-甲基-1H-苯并-1,4-二氮杂卓单盐酸盐 Chemical Name: 7-Bromo-5-(2-chlorophenyl)-2-(methoxymethyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepine
CAS No. 65517-27-3, 61802-93-5 (monoHCl)
项目整合开发状态: Withdrawn
项目研究机构: Kali-Chemie (Originator)
合成路线:Metaclazepam can be prepared by a cyclization reaction of the acyl diamine (I) with phosphorus oxychloride,thus yielding a mixture of two isomeric compounds (II) and (III).This mixture is directly converted into 1-methyl-2-methoxymethyl-5-(2'-chlorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (IV) by means of sodium methoxide in methanol.The nucleophilic attack of the methoxide ion on compound (III) affords nearly complete ring contraction to form (IV) as the main product.Finally,(IV) is halogenated by treatment with N-bromosuccinimide in methylene chloride at reflux temperature.
📌 参考资料/链接：
参考文献标题:Process for making benzodiazepine derivatives
文献作者:Milkowski,W.; Budden,R.; Funke,S.; Hueschens,R.; Liepmann,H.; Stuehmer,W.; Zeugner,H.(Kali-Chemie AG)
参考来源:US 4098786
📄 详细内容
合成路线:Metaclazepam can be prepared by a cyclization reaction of the acyl diamine (I) with phosphorus oxychloride,thus yielding a mixture of two isomeric compounds (II) and (III).This mixture is directly converted into 1-methyl-2-methoxymethyl-5-(2'-chlorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (IV) by means of sodium methoxide in methanol.The nucleophilic attack of the methoxide ion on compound (III) affords nearly complete ring contraction to form (IV) as the main product.Finally,(IV) is halogenated by treatment with N-bromosuccinimide in methylene chloride at reflux temperature.
参考文献标题:Metaclazepam
文献作者:Ruhland,M.; Engelbart,S.; Zeugner,H.
参考来源:Drugs Fut 1982,7(8),577
产品链接: CAS No. 65517-27-3›› 产品链接: CAS No.61802-93-5››