Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (12): 3278-3285.DOI: 10.6023/cjoc201804020 Previous Articles     Next Articles



张平竹, 王晓芬, 郑雪阳, 连平平, 魏超, 李小六   

  1. 河北大学化学与环境科学学院 河北省化学生物学重点实验室 河北大学药物化学与分子诊断教育部重点实验室 保定 071002
  • 收稿日期:2018-04-11 修回日期:2018-07-19 发布日期:2018-08-14
  • 通讯作者: 李小六
  • 基金资助:


Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

Zhang Pingzhu, Wang Xiaofen, Zheng Xueyang, Lian Pingping, Wei Chao, Li Xiaoliu   

  1. Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, School of Chemistry and Environmental Science, Hebei University, Baoding 071002
  • Received:2018-04-11 Revised:2018-07-19 Published:2018-08-14
  • Contact: 10.6023/cjoc201804020
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21572044, 21372060, 21172051), Hebei Natural Science Foundation (No. B2016201031) and Program for Changjiang Scholars and Innovative Research Team in University (No. IRT-15R43), the Colleges and Universities Science Technology Research Project of Hebei Province (No. QN2017015).

A series of novel aryl-substituted imidazo[1,2-a]pyrimidine and triazolo[1,5-a] pyrimidine were synthesized by the tandem reaction of Knoevenagel and Atwal modified Biginelli, following by aromatization. Some of their cytotoxic activities against Hela and A549 cells and inhibition for apple tree canker were preliminarily evaluated.

Key words: Knoevenagel reaction, Biginelli reaction, imidazo[1,2-a]dihypyrimidine, imidazo[1,2-a]pyrimidine, triazolo[1,5-a]pyrimidine