7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓的合成工艺改进  

Improved Synthesis of 7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine

作　　者：陈旭[1] 王平保[2] 穆帅[3] 刘登科[2] 

机构地区：[1]河南大学药学院,河南开封475001 [2]天津药物研究院,天津300193 [3]天津大学化工学院,天津300072

出　　处：《精细化工中间体》2011年第5期27-28,31,共3页Fine Chemical Intermediates

基　　金：天津市科技计划项目(09ZCKFSH01300)

摘　　要：以7-氯-5-氧代-4-乙氧羰基-1-对甲苯磺酰基-2,3,4,5-四氢-1-苯并氮杂卓为原料,在硫酸作用下"一锅法"反应制得7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓。系统研究了硫酸浓度和物料配比对产品收率的影响。总收率为95%。改进后的合成方法操作简单,经济合理,适于工业化生产。The title compound was synthesized in 95% yield from ethyl 7-chloro-5-oxo-1-tosyl-2,3,4,5- tetrahydro-lH-benzo [b] azepine-4-carboxylate in one-step reaction in sulfuric acid. The effects of the concentration of sulfuric acid and the ratio of the reactants were studied. The synthetic process has advantages of simple operation, convenient manipulation and scalable.

关 键 词：7-氯-5-氧代-2 3 4 5-四氢-1H-1-苯并氮杂卓 工艺改进 托伐普坦 

分 类 号：O626.5[理学—有机化学]