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O-去甲文拉法辛的合成工艺研究 被引量:2

Process research on synthesis of O-desmethylvenlafaxine
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摘要 O-去甲文拉法辛是一种新型的抗抑郁药。以4-羟基苯乙酰胺和溴化苄作为起始原料,经缩合、脱水反应后得到4-苄氧基苯乙腈,该中间体与环己酮进行亲核加成后再经还原、甲基化、脱保护等一系列反应最终生成O-去甲文拉法辛。本路线所用原料易得,反应条件温和,工艺操作简便,适合工业化生产。 O-Desmethylvenlafaxine is a new antidepressants. With (4-hydroxyphenyl)acetamide and benzyl bro- mide as the starting materials, 2-(4-(benzyloxy)phenyl)acetonitrile was got after condensation and dehydration. Then it reacted with cyctohexanone by nucleophilic addition reaction. Finally O-desmethylvenlafaxine was obtained after a series of reduction, methylation, deprotection reactions. The raw material of the route is easy to get, and the reaction conditions are mild. The operation is simple, and it is suitable for industrial production.
出处 《精细与专用化学品》 CAS 2015年第8期24-26,共3页 Fine and Specialty Chemicals
关键词 O-去甲文拉法辛 抗抑郁药 合成 O-desmethylvenlafaxine antidepressants synthesis
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  • 1Deecher D C, Beyer C E, Johnston G, et al. Desvenlafaxine succinate: a new serotonin and norepinephrine reuptake inhibi- tor[J]. J PharmacolExpTher, 2006, 318(2)= 657-665.
  • 2Perry R, Cassagnol M. Desvenlafaxine: a new serotonin-norepi- nephrine reuptake inhibitor for the treatment of adults with ma- jor depressive disorder[J]. Clin Ther. 2009, 31(1) 1374 1404.
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