Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (11): 2972-2977.DOI: 10.6023/cjoc201705038 Previous Articles     Next Articles



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;
  • 基金资助:


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;
  • 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).

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