一种微波促进/辅助快速制备联芳基七元内酯的方法。
A Microwave-Promoted/Assisted Method for Rapid Preparation of Biaryl Seven-membered Lactones.
作者信息
Hu Chunqi, Li Jun, Du Wenting
机构信息
College of Chemistry & Chemical Engineering, Shaoxing University, Shaoxing 312000, China.
Department of Pharmacy, Hangzhou Medical College, 481 Binwen Road, Hangzhou 310053, China.
出版信息
Med Chem. 2017;13(3):301-305. doi: 10.2174/1573406413666161117121441.
BACKGROUND
Biaryl seven-membered lactones (BSLs), the target compounds are a class of bioactive compounds with anti-arrhythmic activity, which also serve as a starting material or structural units for chemical synthesis.
OBJECTIVE
To report a simple and efficient procedure for the synthesis of biaryl seven-membered lactones.
METHOD
Under microwave, the umpolung reaction was promoted by N-heterocyclic carbenes under oxygen, with anhydrous potassium carbonate as base and with 1,4,7,10,13,16-Hexanoxacyclooctadecane (18-crown-6) as a phase-transfer catalyst.
RESULTS
The practical protocol was found to be compatible with different structurally diverse substrates and with moderate to excellent yields.
CONCLUSION
This synthesis method has the advantage of high efficacy and novelty, short reaction time, operation simplicity, mild condition and high yields, providing a useful and atom-economic approach to the synthesis of BSLs.
背景
联芳基七元内酯（BSLs），即目标化合物，是一类具有抗心律失常活性的生物活性化合物，同时也是化学合成的起始原料或结构单元。
目的
报道一种简单高效的联芳基七元内酯合成方法。
方法
在微波条件下，以N-杂环卡宾为促进剂，无水碳酸钾为碱，1,4,7,10,13,16-六氧杂环十八烷（18-冠-6）为相转移催化剂，在氧气存在下进行极性翻转反应。
结果
该实用方案被发现与不同结构多样的底物兼容，产率中等至优异。
结论
该合成方法具有高效新颖、反应时间短、操作简便、条件温和、产率高的优点，为联芳基七元内酯的合成提供了一种有用且原子经济的方法。
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