Chinese Journal of Organic Chemistry ›› 2021, Vol. 41 ›› Issue (2): 833-841.DOI: 10.6023/cjoc202007027 Previous Articles     Next Articles



张帆a,b, 侯慧青b, 许秀枝b, 陈志涛b, 柯方b,*()   

  1. a 福建医科大学附属第一医院肿瘤内科 福州 350005
    b 福建医科大学药学院 福建省天然药物药理学重点实验室 福州 350004
  • 收稿日期:2020-07-09 修回日期:2020-08-20 发布日期:2020-09-16
  • 通讯作者: 柯方
  • 作者简介:
    * Corresponding author. E-mail:
  • 基金资助:
    福建省自然科学基金(2016Y9052); 福建省自然科学基金(2016Y9053); 福建省自然科学基金(2017J01820); 福建省自然科学基金(FJNMP-201902); 福建省自然科学基金(2017-1-64)

Visible-Light-Induced Preparation of Quinazolinones by Oxidation of Benzyl Alcohols in Water

Fan Zhanga,b, Huiqing Houb, Xiuzhi Xub, Zhitao Chenb, Fang Keb,*()   

  1. a Department of Medical Oncology, The First Affiliated Hospital of Fujian Medical University, Fuzhou 350005
    b Fujian Provincial Key Laboratory of Natural Medicine Pharmacolog, Department of Pharmacy, Fujian Medical University, Fuzhou 350004
  • Received:2020-07-09 Revised:2020-08-20 Published:2020-09-16
  • Contact: Fang Ke
  • Supported by:
    the Natural Science Foundation of Fujian Province(2016Y9052); the Natural Science Foundation of Fujian Province(2016Y9053); the Natural Science Foundation of Fujian Province(2017J01820); the Natural Science Foundation of Fujian Province(FJNMP-201902); the Natural Science Foundation of Fujian Province(2017-1-64)

A novel visible-light-introduced reaction for the construction of quinazolinone derivatives via radical cyclization of 2-aminobenzamides with benzyl alochols under water phase has been developed. The reaction has been achieved in high yield under mild conditions by using I2 as photocatalyst, which is cheap, available and easy to handle. A variety of quinazolinones were obtained in yields up to 92%. It might provide a promising protocol for the synthesis of quinazolinone derivatives. Its application was performed by the synthesis of N-(2-fluoro-5-methylphenyl)-6-(2,2,2-trifluoroethoxy)pteridin-4-amine, which displayed significant inhibitory activity.

Key words: visible light, Iodine, quinazolinone, oxidant, catalyst