Citation: Zhang Pingzhu, Wang Xiaofen, Zheng Xueyang, Lian Pingping, Wei Chao, Li Xiaoliu. Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives[J]. Chinese Journal of Organic Chemistry, ;2018, 38(12): 3278-3285. doi: 10.6023/cjoc201804020 shu

Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

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

Corresponding author: Li Xiaoliu, lixl@hbu.cn
Received Date: 11 April 2018
Revised Date: 19 July 2018
Available Online: 14 December 2018
Fund Project: 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)the Colleges and Universities Science Technology Research Project of Hebei Province QN2017015Program for Changjiang Scholars and Innovative Research Team in University IRT-15R43the National Natural Science Foundation of China 21172051Hebei Natural Science Foundation B2016201031the National Natural Science Foundation of China 21572044the National Natural Science Foundation of China 21372060

Figures(4)

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.
- Knoevenagel reaction,
- Biginelli reaction,
- imidazo[1, 2-a]dihypyrimidine,
- imidazo[1, 2-a]pyrimidine,
- triazolo[1, 5-a]pyrimidine
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