| 王晶晶,赵鑫雨,何明,吕英涛,康从民.化学通报,2019,82(1):92-95. |
| 苯并呋喃-3-甲酸乙酯的合成方法改进 |
| Improved Synthesis ofEthyl Benzofuran-3-Carboxylate |
| 投稿时间：2018-05-31 修订日期：2018-09-01 |
| DOI： |
| 中文关键词: 邻碘苯酚 丙炔酸乙酯 苯并呋喃-3-甲酸乙酯 一锅法 |
| 英文关键词:o-Iodophenol Ethyl propiolate ethyl Ethyl benzofuran-3-carboxylate One pot synthesis |
| 基金项目:国家自然科学基金项目（NO.21272131）和国家海洋局海洋生物活性物质与现代分析技术重点实验室项目（MBSMAT-2017-06）资助 |
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| 中文摘要: |
| 苯并呋喃骨架广泛存在于天然产物与合成药物中，许多苯并呋喃类衍生物具有重要的生理、药理和毒理学活性，其合成方法备受人们的关注。本文通过“一锅法”合成苯并呋喃-3-甲酸乙酯，在Et3N存在下以甲苯作溶剂、邻碘苯酚与丙炔酸乙酯的投料摩尔比1: 1.5，室温反应20 min后加入K2CO3和Pd(OAc)2/PPh3，85°C反应3.5 h，产率达到78%。本方法避免了反应过程中使用毒性较大的重氮类化合物，反应步骤少，时间短，操作简便，产率较高，并且可以较方便地对目标分子进行结构改变和修饰，对类似化合物的合成具有指导作用。 |
| 英文摘要: |
| The benzofuran skeleton widely exists in natural products and synthetic medicines. Many benzofuran derivatives have important physiological, pharmacological and toxicological activities, and their synthesis methods attracted much attention. A method of "one pot" synthesis ethyl benzofuran-3-carboxylate was obtained: in the presence of Et3N, toluene was used as a solvent, the mole ratio of o-iodophenol to ethyl propiolate was 1:1.5, and the reaction was carried out at room temperature for 20 min; then adding K2CO3, Pd(OAc)2/PPh3 85°C for 3.5 h, the product yield reached 78%. By improving the synthesis method, the process avoids the use of highly toxic diazo compound, and has the advantages of less step, short time, simple operation and high yield. The method reported in this paper hasimplications for the synthesis of similar compounds. |
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