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7-甲氧基-1-萘满酮的合成工艺改进

Improved Synthesis of 7-methoxy-1-tetralone

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【作者】 田雪李昕昊张为革

【Author】 Tian Xue;Li Xinhao;Zhang Weige;College of Pharmaceutical Engineering, Shenyang Pharmaceutical University;Liaoning Benyuan Pharmacy Co., Ltd.;

【通讯作者】 张为革;

【机构】 沈阳药科大学制药工程学院辽宁本源制药有限公司

【摘要】 7-甲氧基-1-萘满酮是合成新型抗抑郁药物阿戈美拉汀的关键中间体,本文以苯甲醚为起始原料,经傅克酰基化、沃尔夫黄鸣龙还原、关环脱水共3步反应合成目标化合物,其结构经1H-NMR、MS谱确证。改进后的合成方法较原工艺路线更简便经济,适合工业化生产。总收率由文献报道的37%提高到58%。

【Abstract】 7-Methoxy-1-tetralone is a key intermediate in the synthesis of new antidepressant agomelatine. In this paper, an anisole was used as the starting material to synthesize the target compound by three-step reaction of Friedel-Crafts acylation, Wolff Huang Ming long reduction and dehydration. Their structures were confirmed by 1 H-NMR and MS spectra. The improved synthesis method is simpler and more economic than the original process route and is suitable for industrial production. The total yield increased from 37 % reported in the literature to 58 %.

【关键词】 7-甲氧基-1-萘满酮合成工艺改进
【Key words】 7-Methoxy-1-tetralonesynthesisImproved
  • 【文献出处】 广东化工 ,Guangdong Chemical Industry , 编辑部邮箱 ,2018年20期
  • 【分类号】TQ460.1
  • 【下载频次】177
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