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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 被引量:1

Improved Synthesis of 7-Chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine
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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.
出处 《精细化工中间体》 CAS 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)
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 7-chloro-5-oxo-2,3,4,5-tetrahydro- 1H- 1-benzazepine improved synthesis Tolvaptan
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