第 46 卷第 5 期Vol. 46 No. 5
2016 年 10 月Oct 2016

所属栏目:医药及中间体

3,4-二羟基苯乙酮的合成
丁华琴,张玉娇,蒋旭亮* (沈阳药科大学 制药工程学院,辽宁 沈阳 110016)
摘 要:研究了邻苯二酚在不同条件下的Friedel-Crafts乙酰化反应。利用三氟化硼乙醚溶液作催化剂,乙酸为乙酰化试剂,合成了3,4-二羟基苯乙酮,并在此基础上,进一步对反应条件进行了优化。优化的条件为:n(三氟化硼)∶n(邻苯二酚)=1.2∶1.0,反应温度为80℃,反应时间为4 h,优化条件下,3,4-二羟基苯乙酮的收率达66.7%。
关键词:3,4-二羟基苯乙酮;三氟化硼;乙酸;乙酰化反应
中图分类号:O625.42  文献标识码:A  文章编号:1009-9212(2016)05-0025-02
Synthesis of 3,4-Dihydroxyacetophenone
DING Hua-qin, ZHANG Yu-jiao, JIANG Xu-liang* (College of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:Friedel-Crafts acetylation reaction of catechol under different conditions was studied. 3,4-Dihydroxyacetophenone was synthesized using boron trifluoride/ethyl ether solution as catalyst and acetic acid as acetylation reagent, and the reaction conditions were further optimized. The optimized reaction conditions were as following: the molar ratio of BF3 to catechol was of 1.2; and the reaction temperature and time were 80℃ and 4 h, respectively. Under the optimized conditions, 3,4-dihydroxyacetophenone was obtained with a yield of 66.7%.
Key words:3,4-dihydroxyacetophenone; boron trifluoride; acetic acid; acetylation reaction
作者简介:丁华琴(1992-),女,江苏东台人,硕士研究生,研究方向:抗肿瘤药物的开发与研究。
联 系 人: 蒋旭亮,副教授,研究方向:新药的设计、合成与活性研究(E-mail:xuliangjiang1975@163.com)。
收稿日期:2016-09-26