有机化学 ›› 2017, Vol. 37 ›› Issue (11): 2972-2977.DOI: 10.6023/cjoc201705038 上一篇    下一篇

研究论文

一步法合成异喹啉酮类化合物

王保取, 孔令斌, 罗琴, 林军, 严胜骄   

  1. 云南大学化学科学与工程学院 教育部自然资源药物化学重点实验室 昆明 650091
  • 收稿日期:2017-05-27 修回日期:2017-07-06 发布日期:2017-07-18
  • 通讯作者: 林军, 严胜骄 E-mail:linjun@ynu.edu.cn;yansj@ynu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21362042,21662042,U1202221,21262042)、云南省自然科学基金(No.2017FA003)、云南省后备人才(No.2012HB001)、云南大学东陆学者及云南大学青年英才计划(No.XT412003)资助项目.

One-Step Synthesis of Isoquinolinone Compounds

Wang Baoqu, Kong Lingbin, Luo Qin, Lin Jun, Yan Shengjiao   

  1. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091
  • Received:2017-05-27 Revised:2017-07-06 Published:2017-07-18
  • Contact: 10.6023/cjoc201705038 E-mail:linjun@ynu.edu.cn;yansj@ynu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21362042, 21662042, U1202221, 21262042), the Natural Science Foundation of Yunnan Province (No. 2017FA003), the Talent Found in Yunnan Province (No. 2012HB001), the Donglu Scholar of Yunnan University and the Excellent Young Talents in Yunnan University (No. XT412003).

建立了一步法简洁、高效合成异喹啉酮类化合物的方法.该方法是利用硝基取代的邻氟苯甲酸甲酯1与杂环烯酮缩胺(HKAs,2)在1,4-二氧六环溶剂中Cs2CO3催化下,加热回流反应.从而实现一步合成异喹啉酮类化合物3.该方法具有合成原料易得、操作简单、路线简洁等特点.

关键词: 环境友好, 原子经济, 杂环烯酮缩胺, 异喹啉酮

A concise and efficiently route for the synthesis of isoquinolinones via one-step reaction of nitro substituted methyl 2-fluorobenzoate 1 and heterocyclic ketone aminals (HKAs, 2) in 1,4-dioxane catalyzed by Cs2CO3 under reflux conditions has been developed. Isoquinolinones 3 were obtained by one-step strategy. This protocol possesses some advantages including readily available starting materials, simple operation and concise synthetic route and so on.

Key words: environment friendly, atom economy, heterocyclic ketone aminals, isoquinolinones